Updated on 2024/04/04
博士（薬学） （ 2002.3 東京大学 ）
創薬科学
organic chemistry
有機合成化学
天然物化学
医薬化学
Nanotechnology/Materials / Synthetic organic chemistry
Life Science / Pharmaceutical chemistry and drug development sciences / 天然物化学
Nagoya University Professor
2017.4
Country：Japan
Nagoya University Associate professor
2012.4 - 2017.3
Country：Japan
The University of Tokyo Associate professor
2011.4 - 2012.3
Country：Japan
The University of Tokyo Lecturer
2008.4 - 2011.3
Country：Japan
The University of Tokyo Assistant Professor
2007.4 - 2008.3
Country：Japan
The University of Tokyo Assistant
2004.4 - 2007.3
Country：Japan
三菱ウェルファーマ株式会社
2002.4 - 2004.3
Country：Japan
日本薬学会
有機合成化学協会
日本化学会
アメリカ化学会
公益社団法人 日本薬学会 理事
2019.3 - 2021.3
Committee type：Academic society
公益社団法人 日本薬学会 医薬化学部会 常任世話人
2018
Committee type：Academic society
公益社団法人 日本薬学会 医薬化学部会 創薬ニューフロンティア検討会メンバー
2018
Committee type：Academic society
公益社団法人 日本薬学会 東海支部幹事
2017
Committee type：Academic society
天然有機化合物討論会 世話人
2017
Committee type：Academic society
有機合成化学協会 編集委員
2014 - 2015
Committee type：Academic society
天然物化学談話会 世話人代表
2011 - 2017
Committee type：Academic society
有機合成化学協会 事業委員
2008 - 2012
天然物化学談話会 世話人
2005 - 2017
日本薬学会 ファルマシア トピックス小委員
2005 - 2007
Committee type：Academic society
Asian Core Program Lectureship Award (China)
2013 Asian Core Program
Asian Core Program Lectureship Award (Singapore)
2013 Asian Core Program
日本薬学会奨励賞
2012.3 日本薬学会
Thieme Journal Award 2010
2010 Thieme
天然物化学談話会奨励賞
2009.7 天然物化学談話会
日本薬学会メディシナルケミストリーシンポジウムポスター賞
2006.12 日本薬学会医薬化学部会
天然有機化合物討論会奨励賞
2001 天然有機化合物討論会
Total Synthesis of Putative Melognine. Reviewed
2024.3
Deep learning driven de novo drug design based on gastric proton pump structures. Reviewed
Abe K, Ozako M, Inukai M, Matsuyuki Y, Kitayama S, Kanai C, Nagai C, Gopalasingam CC, Gerle C, Shigematsu H, Umekubo N, Yokoshima S, Yoshimori A
Communications biology Vol. 6 ( 1 ) page： 956 2023.9
Total syntheses of macleanine and lycoposerramine-S. Reviewed
Okuyama M, Umekubo N, Akimoto K, Shimizu T, Kubokoya K, Nakajima N, Nishiyama Y, Yokoshima S
Organic & biomolecular chemistry Vol. 21 ( 31 ) page： 6289 - 6292 2023.8
Total Syntheses of Malettinins C and E. Reviewed
Umekubo N, Yokoshima S
Organic letters Vol. 25 ( 24 ) page： 4530 - 4533 2023.6
Construction of the tetracyclic ring system of diterpene alkaloids via cationic [5 + 2] cycloaddition. Reviewed
Mizuno K, Nishiyama Y, Yokoshima S
Organic & biomolecular chemistry Vol. 21 ( 22 ) page： 4587 - 4590 2023.6
Total Synthesis of Kopsone. Reviewed
Tomoya K, Komiya K, Nakajima D, Umekubo N, Yokoshima S
Organic letters Vol. 25 ( 15 ) page： 2718 - 2721 2023.4
Fluorinated 2,6-Xylenesulfonyl Group: A Protective Group for Amines. Reviewed
Katayama Y, Watanabe K, Nishiyama Y, Yokoshima S
Organic letters Vol. 25 ( 8 ) page： 1326 - 1330 2023.3
Convergent synthesis of the [5-7-6-3] tetracyclic core of premyrsinane diterpenes. Reviewed
Yoshinaga K, Yokoshima S
Organic & biomolecular chemistry Vol. 21 ( 4 ) page： 724 - 727 2023.1
Construction of the [7-5-5] Tricyclic Core of Daphniphyllum Alkaloids via a Cationic Cascade Reaction. Reviewed
Nakajima D, Yokoshima S
Organic letters Vol. 24 ( 51 ) page： 9520 - 9524 2022.12
Formal Synthesis of Ecteinascidin 743 via an Intramolecular Cascade Heck Reaction to Construct the Diazabicyclo[3.3.1]nonane Framework. Reviewed
Nakajima N, Yoshida E, Toma T, Nishiyama Y, Inoue M, Fukuyama T, Yokoshima S
Organic letters Vol. 24 ( 44 ) page： 8228 - 8232 2022.11
Anticancer Approach Inspired by the Hepatotoxic Mechanism of Pyrrolizidine Alkaloids with Glycosylated Artificial Metalloenzymes. Reviewed
Kurimoto M, Chang TC, Nishiyama Y, Suzuki T, Dohmae N, Tanaka K, Yokoshima S
Angewandte Chemie (International ed. in English) Vol. 61 ( 43 ) page： e202205541 2022.10
Photoinduced rearrangement of α-(2-nitrophenyl)ketones. Reviewed
Kitayama S, Shimizu H, Yokoshima S
Organic & biomolecular chemistry Vol. 20 ( 40 ) page： 7896 - 7899 2022.10
Substitution of α-Azido Sulfones with Thiolates to Form α-Azido Sulfides. Reviewed
Katayama A, Jin Y, Nishiyama Y, Hosoya T, Yokoshima S
Organic letters Vol. 24 ( 40 ) page： 7361 - 7365 2022.10
Synthetic Approach toward (-)-Tetrodotoxin via Construction of the Bicyclo[2.2.2]octane Skeleton Reviewed
Kobayashi Kazuki, Senoo Yoshiki, Toma Tatsuya, Fukuyama Tohru, Yokoshima Satoshi
SYNLETT Vol. 33 ( 04 ) page： 391 - 395 2022.3
Photo-oxygenation by a biocompatible catalyst reduces amyloid-β levels in Alzheimer's disease mice. Reviewed
Ozawa S, Hori Y, Shimizu Y, Taniguchi A, Suzuki T, Wang W, Chiu YW, Koike R, Yokoshima S, Fukuyama T, Takatori S, Sohma Y, Kanai M, Tomita T
Brain : a journal of neurology Vol. 144 ( 6 ) page： 1884 - 1897 2021.7
Total Synthesis of Haliclonin A. Reviewed
Jin Y, Orihara K, Kawagishi F, Toma T, Fukuyama T, Yokoshima S
Angewandte Chemie (International ed. in English) Vol. 60 ( 17 ) page： 9666 - 9671 2021.4
Nitrone Formation by Reaction of an Enolate with a Nitro Group. Reviewed
Shimizu H, Yoshinaga K, Yokoshima S
Organic letters Vol. 23 ( 7 ) page： 2704 - 2709 2021.4
A novel translation inhibitor, mersicarpine, inhibits S-phase progression and induces apoptosis in HL60 cells. Reviewed
Shiobara T, Nagumo Y, Nakajima R, Fukuyama T, Yokoshima S, Usui T
Bioscience, biotechnology, and biochemistry Vol. 85 ( 1 ) page： 92 - 96 2021.1
Synthesis of 2-Azabicyclo[3.3.1]nonanes: Lessons from Synthetic Studies of Macrocyclic Diamine Alkaloids Invited Reviewed
Yokoshima Satoshi
CHEMISTRY LETTERS Vol. 50 ( 1 ) page： 96 - 102 2021.1
Copper-Mediated Conversion of Alkynes into Nitriles via Iodotriazoles. Reviewed
Kori R, Murakami K, Nishiyama Y, Toma T, Yokoshima S
Chemical & pharmaceutical bulletin Vol. 69 ( 3 ) page： 278 - 280 2021
SYNTHETIC STUDIES ON DENSANINS: STEREOSELECTIVE CONSTRUCTION OF A PYRROLIDINE RING CONTAINING A QUATERNARY CARBON Reviewed
Ueda Kyosuke, Yokoshima Satoshi
HETEROCYCLES Vol. 103 ( 1 ) page： 172 - 176 2021
Synthesis of Polycyclic Natural Products through Skeletal Rearrangement Invited Reviewed
Yokoshima Satoshi
SYNLETT Vol. 31 ( 20 ) page： 1967 - 1975 2020.12
Structure-Activity Relationship Study of Majusculamides A and B and Their Analogues on Osteogenic Activity Reviewed
Natsume Noriyuki, Ozaki Kaori, Nakajima Daisuke, Yokoshima Satoshi, Teruya Toshiaki
JOURNAL OF NATURAL PRODUCTS Vol. 83 ( 8 ) page： 2477 - 2482 2020.8
Semipinacol Rearrangement Induced by Cleavage of Dibromocyclopropane Reviewed
Kurimoto Michitaka, Nakajima Daisuke, Nishiyama Yoshitake, Yokoshima Satoshi
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY Vol. 2020 ( 27 ) page： 4108 - 4111 2020.7
Total Synthesis of Tetrodotoxin Reviewed
Murakami Keigo, Toma Tatsuya, Fukuyama Tohru, Yokoshima Satoshi
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION Vol. 59 ( 15 ) page： 6253 - 6257 2020.4
Synthetic Studies on Bilobalide
Shiogai Akihiro, Toma Tatsuya, Yokoshima Satoshi
SYNLETT Vol. 31 ( 3 ) page： 290 - 294 2020.2
An artificial metalloenzyme biosensor can detect ethylene gas in fruits and Arabidopsis leaves
Vong Kenward, Eda Shohei, Kadota Yasuhiro, Nasibullin Igor, Wakatake Takanori, Yokoshima Satoshi, Shirasu Ken, Tanaka Katsunori
NATURE COMMUNICATIONS Vol. 10 ( 1 ) page： 5746 2019.12
Synthesis of Majusculamides A and B Reviewed
Nakajima Daisuke, Sueyoshi Kosuke, Orihara Kensuke, Teruya Toshiaki, Yokoshima Satoshi
SYNLETT Vol. 30 ( 8 ) page： 924 - 927 2019.5
PREFACE TO HETEROCYCLES ISSUE HONORING THE 70TH BIRTHDAY OF PROFESSOR TOHRU FUKUYAMA
Yokoshima Satoshi
HETEROCYCLES Vol. 99 ( 1 ) page： 1 - 3 2019.4
Synthetic Studies of Isoschizogamine: Alternative Preparation of the Key Intermediate.
Hayashi N, Miura Y, Yokoshima S, Fukuyama T
Chemical & pharmaceutical bulletin Vol. 67 ( 1 ) page： 64 - 70 2019.1
天然物合成がもたらす新たな骨格構築と創薬 Invited Reviewed
横島 聡
MEDCHEM NEWS Vol. 29 ( 4 ) page： 178 - 182 2019
Total Synthesis of Lycoposerramine-R
Watanabe Shinya, Ishikawa Masatsugu, Nomura Toshimune, Fukuyama Tohru, Yokoshima Satoshi
SYNLETT Vol. 29 ( 18 ) page： 2377-2380 2018.11
Synthetic Studies of the Daphniphyllum Alkaloids: A Cooperative Reaction of Proximal Functional Groups Forming a Tetracyclic System
Yamada Ryosuke, Fukuyama Tohru, Yokoshima Satoshi
ORGANIC LETTERS Vol. 20 ( 15 ) page： 4504 - 4506 2018.8
A small-molecule inhibitor of SOD1-Derlin-1 interaction ameliorates pathology in an ALS mouse model
Tsuburaya Naomi, Homma Kengo, Higuchi Tsunehiko, Balia Andrii, Yamakoshi Hiroyuki, Shibata Norio, Nakamura Seiichi, Nakagawa Hidehiko, Ikeda Shin-ichi, Umezawa Naoki, Kato Nobuki, Yokoshima Satoshi, Shibuya Masatoshi, Shimonishi Manabu, Kojima Hirotatsu, Okabe Takayoshi, Nagano Tetsuo, Naguro Isao, Imamura Keiko, Inoue Haruhisa, Fujisawa Takao, Ichijo Hidenori
NATURE COMMUNICATIONS Vol. 9 ( 1 ) page： 2668 2018.7
Synthesis of the [7-5-5] tricyclic core of Daphniphyllum alkaloids
Kitabayashi Yusuke, Fukuyama Tohru, Yokoshima Satoshi
ORGANIC & BIOMOLECULAR CHEMISTRY Vol. 16 ( 19 ) page： 3556 - 3559 2018.5
Synthetic Studies of Haliclonin A: Construction of the 3-Azabicyclo[3.3.1]nonane Skeleton with a Bridge that Forms the 17-Membered Ring
Orihara Kensuke, Kawagishi Fumiki, Yokoshima Satoshi, Fukuyama Tohru
SYNLETT Vol. 29 ( 6 ) page： 769-772 2018.4
Total synthesis of (+)-lysergic acid Reviewed
Kanno Rentaro, Yokoshima Satoshi, Kanai Motomu, Fukuyama Tohru
JOURNAL OF ANTIBIOTICS Vol. 71 ( 2 ) page： 240-247 2018.2
Total Synthesis of Huperzine R Reviewed
Nomura Toshimune, Yokoshima Satoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 20 ( 1 ) page： 119-121 2018.1
Synthesis of Cardiopetaline via a Wagner-Meerwein Rearrangement without Preactivation of the Pivotal Hydroxy Group Reviewed
Nishiyama Yoshitake, Yokoshima Satoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 19 ( 21 ) page： 5833-5835 2017.11
Synthesis of Lycopodium Alkaloids Reviewed
Yokoshima Satoshi
JOURNAL OF SYNTHETIC ORGANIC CHEMISTRY JAPAN Vol. 75 ( 10 ) page： 1035-1044 2017.10
Discovery of novel 2-(3-phenylpiperazin-1-yl)-pyrimidin-4-ones as glycogen synthase kinase-3 beta inhibitors Reviewed
Usui Yoshihiro, Uehara Fumiaki, Hiki Shinsuke, Watanabe Kazutoshi, Tanaka Hiroshi, Shouda Aya, Yokoshima Satoshi, Aritomo Keiichi, Adachi Takashi, Fukunaga Kenji, Sunada Shinji, Nabeno Mika, Saito Ken-Ichi, Eguchi Jun-ichi, Yamagami Keiji, Asano Shouichi, Tanaka Shinji, Yuki Satoshi, Yoshii Narihiko, Fujimura Masatake, Horikawa Takashi
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS Vol. 27 ( 16 ) page： 3726-3732 2017.8
Total Synthesis of Huperzine Q Reviewed
Tanimura Shun, Yokoshima Satoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 19 ( 13 ) page： 3684-3686 2017.7
High-throughput Screening of Small Molecule Inhibitors of the Streptococcus Quorum-sensing Signal Pathway Reviewed
Ishii Seiji, Fukui Kenji, Yokoshima Satoshi, Kumagai Kazuo, Beniyama Youko, Kodama Tetsuya, Fukuyama Tohru, Okabe Takayoshi, Nagano Tetsuo, Kojima Hirotatsu, Yano Takato
SCIENTIFIC REPORTS Vol. 7 2017.6
Total Syntheses of Aurachins A and B Reviewed
Hattori Haruhiko, Yokoshima Satoshi, Fukuyama Tohru
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION Vol. 56 ( 24 ) page： 6980-6983 2017.6
Total Synthesis of (-)-Morphine Reviewed
Umihara Hirotatsu, Yokoshima Satoshi, Inoue Masayuki, Fukuyama Tohru
CHEMISTRY-A EUROPEAN JOURNAL Vol. 23 ( 29 ) page： 6993-6995 2017.5
Total Synthesis of (-)-Tetrodotoxin and 11-norTTX-6(R)-ol Reviewed
Maehara Tomoaki, Motoyama Keisuke, Toma Tatsuya, Yokoshima Satoshi, Fukuyama Tohru
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION Vol. 56 ( 6 ) page： 1549-1552 2017.2
Total Synthesis of Lycopalhine A Reviewed
Ochi Yuji, Yokoshima Satoshi, Fukuyama Tohru
SYNTHESIS-STUTTGART Vol. 49 ( 1 ) page： 96-114 2017.1
Chemical Transformation of an Intermediate in the Synthesis of Huperzine A, Leading to a Diverse Array of Molecules Reviewed
Yokoshima Satoshi, Ishikawa Masatsugu, Beniyama Youko, Fukuyama Tohru
CHEMICAL & PHARMACEUTICAL BULLETIN Vol. 64 ( 10 ) page： 1528-1531 2016.10
Eudistomin C, an Antitumor and Antiviral Natural Product, Targets 40S Ribosome and Inhibits Protein Translation Reviewed
Ota Yu, Chinen Takumi, Yoshida Keisuke, Kudo Shun, Nagumo Yoko, Shiwa Yuh, Yamada Ryosuke, Umihara Hirotatsu, Iwasaki Kotaro, Masumoto Hiroshi, Yokoshima Satoshi, Yoshikawa Hirofumi, Fukuyama Tohru, Kobayashi Junichi, Usui Takeo
CHEMBIOCHEM Vol. 17 ( 17 ) page： 1616-1620 2016.9
Morphological Evaluation of Nonlabeled Cells to Detect Stimulation of Nerve Growth Factor Expression by Lyconadin B Reviewed
Kawai Shun, Sasaki Hiroto, Okada Norihiro, Kanie Kei, Yokoshima Satoshi, Fukuyama Tohru, Honda Hiroyuki, Kato Ryuji
JOURNAL OF BIOMOLECULAR SCREENING Vol. 21 ( 8 ) page： 795-803 2016.9
BIN1 regulates BACE1 intracellular trafficking and amyloid-beta production Reviewed
Miyagawa Toji, Ebinuma Ihori, Morohashi Yuichi, Hori Yukiko, Chang Mee Young, Hattori Haruhiko, Maehara Tomoaki, Yokoshima Satoshi, Fukuyama Tohru, Tsuji Shoji, Iwatsubo Takeshi, Prendergast George C., Tomita Taisuke
HUMAN MOLECULAR GENETICS Vol. 25 ( 14 ) page： 2948-2958 2016.7
Conversion of Vindoline into 11-Mesyloxytabersonine Reviewed
Han-ya Yuki, Inui Tomohiko, Yokoshima Satoshi, Tokuyama Hidetoshi, Fukuyama Tohru
CHEMICAL & PHARMACEUTICAL BULLETIN Vol. 64 ( 7 ) page： 800-804 2016.7
Total Synthesis of (-)-Cardiopetaline Reviewed
Nishiyama Yoshitake, Yokoshima Satoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 18 ( 10 ) page： 2359-2362 2016.5
Total Synthesis of (-)-Daphenylline Reviewed
Yamada Ryosuke, Adachi Yohei, Yokoshima Satoshi, Fukuyama Tohru
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION Vol. 55 ( 20 ) page： 6067-6070 2016.5
Total Synthesis of Lycopalhine A Reviewed
Ochi Yuji, Yokoshima Satoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 18 ( 6 ) page： 1494-1496 2016.3
Synthetic Studies on Huperzine R: Construction of the 1-Azabicyclo[5.4.3]tetradec-6-ene Core Reviewed
Kumazaki Hiroshi, Nakajima Rie, Bessho Yuka, Yokoshima Satoshi, Fukuyama Tohru
SYNLETT Vol. 26 ( 15 ) page： 2131-2134 2015.9
Conversion of Ester Moieties to 4-Bromophenyl Groups via Electrocyclic Reaction of Dibromocyclopropanes Reviewed
Ueda Kyosuke, Umihara Hirotatsu, Yokoshima Satoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 17 ( 13 ) page： 3191-3193 2015.7
Synthetic Studies on Plakinidines Reviewed
Komori Takashi, Yokoshima Satoshi, Fukuyama Tohru
SYNLETT Vol. 26 ( 11 ) page： 1537-1540 2015.7
Formal Synthesis of Sarain A: Intramolecular Cycloaddition of an Eight-Membered Cyclic Nitrone to Construct the 2-Azabicyclo-[3.3.1]nonane Framework Reviewed
Higo Takuya, Ukegawa Tomoya, Yokoshima Satoshi, Fukuyama Tohru
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION Vol. 54 ( 25 ) page： 7367-7370 2015.6
Asymmetric synthesis of 2-arylpiperazines Reviewed
Yokoshima Satoshi, Watanabe Kazutoshi, Uehara Fumiaki, Usui Yoshihiro, Tanaka Hiroshi
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS Vol. 24 ( 24 ) page： 5749-5751 2014.12
Synthesis of (-)-Oxycodone Reviewed
Kimishima Atsushi, Umihara Hirotatsu, Mizoguchi Akihiro, Yokoshima Satoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 16 ( 23 ) page： 6244-6247 2014.12
Total Synthesis of Lysergic Acid (vol 16, pg 1269, 2014) Reviewed
Umezaki Satoshi, Yokoshima Satoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 16 ( 17 ) page： 4692-4692 2014.9
A Unified Strategy for Kainoid Synthesis Reviewed
Fujii Masaya, Yokoshima Satoshi, Fukuyama Tohru
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY ( 22 ) page： 4823-4836 2014.8
Allosteric regulation of gamma-secretase activity by a phenylimidazole-type gamma-secretase modulator Reviewed
Takeo Koji, Tanimura Shun, Shinoda Takehiro, Osawa Satoko, Zahariev Ivan Krasmirov, Takegami Naoki, Ishizuka-Katsura Yoshiko, Shinya Naoko, Takagi-Niidome Shizuka, Tominaga Aya, Ohsawa Noboru, Kimura-Someya Tomomi, Shirouzu Mikako, Yokoshima Satoshi, Yokoyama Shigeyuki, Fukuyama Tohru, Tomita Taisuke, Iwatsubo Takeshi
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA Vol. 111 ( 29 ) page： 10544-10549 2014.7
New photocleavable linker: alpha-Thioacetophenone-type linker Reviewed
Yonezawa Hirotaka, Nishiyama Yoshitake, Takeo Koji, Iwatsubo Takeshi, Tomita Taisuke, Yokoshima Satoshi, Fukuyama Tohru
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS Vol. 24 ( 13 ) page： 2831-2833 2014.7
Total Synthesis of (-)-Lepistine Reviewed
Kitabayashi Yusuke, Yokoshima Satoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 16 ( 11 ) page： 2862-2864 2014.6
Total Synthesis of (-)-Lepenine Reviewed
Nishiyama Yoshitake, Han-ya Yuki, Yokoshima Satoshi, Fukuyama Tohru
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY Vol. 136 ( 18 ) page： 6598-6601 2014.5
Total Synthesis of (-)-Mersicarpine (vol 132, pg 1236, 2010) Reviewed
Nakajima Rie, Ogino Tsuyoshi, Yokoshima Satoshi, Fukuyama Tohru
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY Vol. 136 ( 15 ) page： 5816-5816 2014.4
Concise Total Synthesis of (+)-Lyconadin A (vol 133, pg 418, 2011) Reviewed
Nishimura Takuya, Unni Aditya K., Yokoshima Satoshi, Fukuyama Tohru
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY Vol. 136 ( 15 ) page： 5818-5818 2014.4
Total Synthesis of Ecteinascidin 743 (vol 135, pg 13684, 2013) Reviewed
Kawagishi Fumiki, Toma Tatsuya, Inui Tomohiko, Yokoshima Satoshi, Fukuyama Tohru
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY Vol. 136 ( 15 ) page： 5815-5815 2014.4
Total Syntheses of Lyconadins A-C (vol 135, pg 3243, 2013) Reviewed
Nishimura Takuya, Unni Aditya K., Yokoshima Satoshi, Fukuyama Tohru
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY Vol. 136 ( 15 ) page： 5817-5817 2014.4
Correction of Synthetic Studies on Chartelline C: Stereoselective Construction of the Core Skeleton Reviewed
Iwasaki Kotaro, Kanno Rentaro, Morimoto Toshiharu, Yamashita Tohru, Yokoshima Satoshi, Fukuyama Tohru
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION Vol. 53 ( 15 ) page： 3768-3768 2014.4
Total Synthesis of (-)-Huperzine A (vol 11, pg 5354, 2009) Reviewed
Koshiba Takahiro, Yokoshima Satoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 16 ( 4 ) page： 1270-1270 2014.2
Total Synthesis of Lysergic Acid (vol 15, pg 4230, 2013) Reviewed
Umezaki Satoshi, Yokoshima Satoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 16 ( 4 ) page： 1269-1269 2014.2
(1-Nosyl-5-nitroindol-3-yl)methyl Ester: A Novel Protective Group for Carboxylic Acids (vol 10, pg 2601, 2008) Reviewed
Nishimura Takuya, Yamada Kouhei, Takebe Tohru, Yokoshima Satoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 16 ( 4 ) page： 1268-1268 2014.2
2-Pyridone Synthesis Using 2-(Phenylsulfinyl)acetamide (vol 15, pg 232, 2013) Reviewed
Fujii Masaya, Nishimura Takuya, Koshiba Takahiro, Yokoshima Satoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 16 ( 4 ) page： 1272-1272 2014.2
Total Synthesis of (-)-Histrionicotoxin (vol 13, pg 4466, 2011) Reviewed
Adachi Yohei, Kamei Noriyuki, Yokoshima Satoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 16 ( 4 ) page： 1273-1273 2014.2
Binding of longer A beta to transmembrane domain 1 of presenilin 1 impacts on A beta 42 generation Reviewed
Ohki Yu, Shimada Naoaki, Tominaga Aya, Osawa Satoko, Higo Takuya, Yokoshima Satoshi, Fukuyama Tohru, Tomita Taisuke, Iwatsubo Takeshi
MOLECULAR NEURODEGENERATION Vol. 9 2014.1
Total Synthesis of Ecteinascidin 743 Reviewed
Kawagishi Fumiki, Toma Tatsuya, Inui Tomohiko, Yokoshima Satoshi, Fukuyama Tohru
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY Vol. 135 ( 37 ) page： 13684-13687 2013.9
Total Synthesis of Lysergic Acid Reviewed
Umezaki Satoshi, Yokoshima Satoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 15 ( 16 ) page： 4230-4233 2013.8
Synthesis of Natural Products with Polycyclic Systems Reviewed
Yokoshima Satoshi
CHEMICAL & PHARMACEUTICAL BULLETIN Vol. 61 ( 3 ) page： 251-257 2013.3
Effect of Helical Conformation and Side Chain Structure on gamma-Secretase Inhibition by beta-Peptide Foldamers: Insight into Substrate Recognition Reviewed
Imamura Yuki, Umezawa Naoki, Osawa Satoko, Shimada Naoaki, Higo Takuya, Yokoshima Satoshi, Fukuyama Tohru, Iwatsubo Takeshi, Kato Nobuki, Tomita Taisuke, Higuchi Tsunehiko
JOURNAL OF MEDICINAL CHEMISTRY Vol. 56 ( 4 ) page： 1443-1454 2013.2
Total Syntheses of Lyconadins A-C Reviewed
Nishimura Takuya, Unni Aditya K., Yokoshima Satoshi, Fukuyama Tohru
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY Vol. 135 ( 8 ) page： 3243-3247 2013.2
2-Pyridone Synthesis Using 2-(Phenylsulfinyl)acetamide Reviewed
Fujii Masaya, Nishimura Takuya, Koshiba Takahiro, Yokoshima Satoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 15 ( 1 ) page： 232-234 2013.1
Activity-Dependent Proteolytic Cleavage of Neuroligin-1 Reviewed
Suzuki Kunimichi, Hayashi Yukari, Nakahara Soichiro, Kumazaki Hiroshi, Prox Johannes, Horiuchi Keisuke, Zeng Mingshuo, Tanimura Shun, Nishiyama Yoshitake, Osawa Satoko, Sehara-Fujisawa Atsuko, Saftig Paul, Yokoshima Satoshi, Fukuyama Tohru, Matsuki Norio, Koyama Ryuta, Tomita Taisuke, Iwatsubo Takeshi
NEURON Vol. 76 ( 2 ) page： 410-422 2012.10
Synthetic Studies toward Ecteinascidin 743 (Trabectedin) Reviewed
Imai Takahiro, Nakata Hiyoku, Yokoshima Satoshi, Fukuyama Tohru
SYNTHESIS-STUTTGART Vol. 44 ( 17 ) page： 2743-2753 2012.9
Total Synthesis of (-)-Lemonomycin Reviewed
Yoshida Atsushi, Akaiwa Michinori, Asakawa Tomohiro, Hamashima Yoshitaka, Yokoshima Satoshi, Fukuyama Tohru, Kan Toshiyuki
CHEMISTRY-A EUROPEAN JOURNAL Vol. 18 ( 36 ) page： 11192-11195 2012.9
Total Synthesis of (-)-Isoschizogamine Reviewed
Miura Yusuke, Hayashi Noriyuki, Yokoshima Satoshi, Fukuyama Tohru
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY Vol. 134 ( 29 ) page： 11995-11997 2012.7
A Practical Preparation of Highly Versatile N-Acylpyrroles from 2,4,4-Trimethoxybutan-1-amine Reviewed
Maehara Tomoaki, Kanno Rentaro, Yokoshima Satoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 14 ( 7 ) page： 1946-1948 2012.4
Total Synthesis of (-)-Anisatin Reviewed
Ogura Akihiro, Yamada Kohei, Yokoshima Satoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 14 ( 6 ) page： 1632-1635 2012.3
Identification of novel deoxyribofuranosyl indole antimicrobial agents Reviewed
Paudel Atmika, Hamamoto Hiroshi, Kobayashi Yoshihisa, Yokoshima Satoshi, Fukuyama Tohru, Sekimizu Kazuhisa
JOURNAL OF ANTIBIOTICS Vol. 65 ( 2 ) page： 53-57 2012.2
Total synthesis of gelsemoxonine Reviewed
Shimokawa Jun, Harada Takaaki, Yokoshima Satoshi, Fukuyama Tohru
PURE AND APPLIED CHEMISTRY Vol. 84 ( 7 ) page： 1643-1650 2012
Synthetic Studies on Chartelline C: Stereoselective Construction of the Core Skeleton Reviewed
Iwasaki Kotaro, Kanno Rentaro, Morimoto Toshiharu, Yamashita Tohru, Yokoshima Satoshi, Fukuyama Tohru
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION Vol. 51 ( 36 ) page： 9160-9163 2012
Total Synthesis of (-)-Lycoposerramine-S Reviewed
Shimada Naoaki, Abe Yuzo, Yokoshima Satoshi, Fukuyama Tohru
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION Vol. 51 ( 47 ) page： 11824-11826 2012
A Practical Synthesis of (-)-Kainic Acid Reviewed
Takita Satoshi, Yokoshima Satoshi, Fukuyama Tohru
SYNTHESIS-STUTTGART ( 23 ) page： 3848-3858 2011.12
Phenylpiperidine-type gamma-secretase modulators target the transmembrane domain 1 of presenilin 1 Reviewed
Ohki Yu, Higo Takuya, Uemura Kengo, Shimada Naoaki, Osawa Satoko, Berezovska Oksana, Yokoshima Satoshi, Fukuyama Tohru, Tomita Taisuke, Iwatsubo Takeshi
EMBO JOURNAL Vol. 30 ( 23 ) page： 4815-4824 2011.11
Total Synthesis of Gelsemoxonine Reviewed
Shimokawa Jun, Harada Takaaki, Yokoshima Satoshi, Fukuyama Tohru
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY Vol. 133 ( 44 ) page： 17634-17637 2011.11
Practical synthesis of (-)-kainic acid Reviewed
Takita Satoshi, Yokoshima Satoshi, Fukuyama Tohru
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY Vol. 242 page： . 2011.8
Total Synthesis of (-)-Histrionicotoxin Reviewed
Adachi Yohei, Kamei Noriyuki, Yokoshima Satoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 13 ( 16 ) page： 4446-4449 2011.8
Copper-Mediated Aryl Amination: In Situ Generation of an Active Copper(I) Species Reviewed
Komori Takashi, Satoh Nobuhiro, Yokoshima Satoshi, Fukuyama Tohru
SYNLETT ( 13 ) page： 1859-1862 2011.8
Total Synthesis of (-)-Salinosporamide A Reviewed
Satoh Nobuhiro, Yokoshima Satoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 13 ( 12 ) page： 3028-3031 2011.6
BACE1 Activity Is Modulated by Cell-Associated Sphingosine-1-Phosphate Reviewed
Takasugi Nobumasa, Sasaki Tomoki, Suzuki Kunimichi, Osawa Satoko, Isshiki Hayato, Hori Yukiko, Shimada Naoaki, Higo Takuya, Yokoshima Satoshi, Fukuyama Tohru, Lee Virginia M. -Y., Trojanowski John Q., Tomita Taisuke, Iwatsubo Takeshi
JOURNAL OF NEUROSCIENCE Vol. 31 ( 18 ) page： 6850-6857 2011.5
A Practical Synthesis of (-)-Kainic Acid Reviewed
Takita Satoshi, Yokoshima Satoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 13 ( 8 ) page： 2068-2070 2011.4
Concise Total Synthesis of (+)-Lyconadin A Reviewed
Nishimura Takuya, Unni Aditya K., Yokoshima Satoshi, Fukuyama Tohru
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY Vol. 133 ( 3 ) page： 418-419 2011.1
Let's Challenge Reviewed
Yokoshima Satoshi
JOURNAL OF SYNTHETIC ORGANIC CHEMISTRY JAPAN Vol. 68 ( 12 ) page： 1323-1324 2010.12
Development of photoaffinity probes for gamma-secretase equipped with a nitrobenzenesulfonamide-type cleavable linker (vol 19, pg 6869, 2009) Reviewed
Yokoshima Satoshi, Abe Yuzo, Watanabe Naoto, Kita Yoichi, Kan Toshiyuki, Iwatsubo Takeshi, Tomita Taisuke, Fukuyama Tohru
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS Vol. 20 ( 5 ) page： 1798-1799 2010.3
Total Synthesis of (-)-Mersicarpine Reviewed
Nakajima Rie, Ogino Tsuyoshi, Yokoshima Satoshi, Fukuyama Tohru
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY Vol. 132 ( 4 ) page： 1236-+ 2010.2
Total Synthesis of (-)-Morphine Reviewed
Koizumi Hifumi, Yokoshima Satoshi, Fukuyama Tohru
CHEMISTRY-AN ASIAN JOURNAL Vol. 5 ( 10 ) page： 2192-2198 2010
Total Synthesis of (+)-Vinblastine: Control of the Stereochemistry at C18 ' Reviewed
Yokoshima Satoshi, Tokuyama Hidetoshi, Fukuyama Tohru
CHEMICAL RECORD Vol. 10 ( 2 ) page： 101-118 2010
Development of photoaffinity probes for gamma-secretase equipped with a nitrobenzenesulfonamide-type cleavable linker Reviewed
Yokoshima Satoshi, Abe Yuzo, Watanabe Naoto, Kita Yoichi, Kan Toshiyuki, Iwatsubo Takeshi, Tomita Taisuke, Fukuyama Tohru
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS Vol. 19 ( 24 ) page： 6869-6871 2009.12
Total Synthesis of (-)-Huperzine A Reviewed
Koshiba Takahiro, Yokoshima Satoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 11 ( 22 ) page： 5354-5356 2009.11
A practical synthesis of (-)-oseltamivir Reviewed
Satoh Nobuhiro, Akiba Takahiro, Yokoshima Satoshi, Fukuyama Tohru
TETRAHEDRON Vol. 65 ( 16 ) page： 3239-3245 2009.4
SYNTHETIC STUDIES TOWARD (+)-LYSERGIC ACID: CONSTRUCTION OF THE TETRACYCLIC ERGOLINE SKELETON Reviewed
Inoue Tohru, Yokoshima Satoshi, Fukuyama Tohru
HETEROCYCLES Vol. 79 page： 373-378 2009.4
TOTAL SYNTHESIS OF (+/-)-MORPHINE Reviewed
Uchida Kenji, Yokoshima Satoshi, Kan Toshiyuki, Fukuyama Tohru
HETEROCYCLES Vol. 77 ( 2 ) page： 1219-1234 2009.2
A SIMPLE CHIRAL TEMPLATE FOR THE SYNTHESIS OF FUNCTIONALIZED alpha-ARYLGLYCINE DERIVATIVES Reviewed
Nakata Hiyoku, Imai Takahiro, Yokoshima Satoshi, Fukuyama Tohru
HETEROCYCLES Vol. 76 ( 1 ) page： 747-757 2008.9
(1-nosyl-5-nitroindol-3-yl)methyl ester: A novel protective group for carboxylic acids Reviewed
Nishimura Takuya, Yamada Kouhei, Takebe Tohru, Yokoshima Satoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 10 ( 12 ) page： 2601-2604 2008.6
Synthesis of eudistomin C and E: Improved preparation of the indole unit Reviewed
Yamagishi Hiroaki, Matsumoto Koji, Iwasaki Kotaro, Miyazaki Tohru, Yokoshima Satoshi, Tokuyama Hidetoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 10 ( 12 ) page： 2369-2372 2008.6
Oseltamivir enhances hippocampal network synchronization Reviewed
Usami Atsushi, Sasaki Takuya, Satoh Nobuhiro, Akiba Takahiro, Yokoshima Satoshi, Fukuyama Tohru, Yamatsugu Kenzo, Kanai Motomu, Shibasaki Masakatsu, Matsuki Norio, Ikegaya Yuji
JOURNAL OF PHARMACOLOGICAL SCIENCES Vol. 106 ( 4 ) page： 659-662 2008.4
Oseltamivir induces spike synchronization in hippocampal networks Reviewed
Usami Atsushi, Sasaki Takuya, Satoh Nobuhiro, Akiba Takahiro, Yokoshima Satoshi, Fukuyama Tohru, Yamatsugu Kenzo, Kanai Motomu, Shibasaki Masakatsu, Matsuki Norio, Ikegaya Yuji
JOURNAL OF PHARMACOLOGICAL SCIENCES Vol. 106 page： 173P-173P 2008
Synthesis of (+)-vinblastine and its analogues Reviewed
Miyazaki Tohru, Yokoshirna Satoshi, Simizu Siro, Osada Hiroyuki, Tokuyama Hidetoshi, Fukuyama Tohru
ORGANIC LETTERS Vol. 9 ( 23 ) page： 4737-4740 2007.11
A practical synthesis of (-)-Oseltamivir Reviewed
Satoh Nobuhiro, Akiba Takahiro, Yokoshima Satoshi, Fukuyama Tohru
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION Vol. 46 ( 30 ) page： 5734-5736 2007
Diastereoselective synthesis of atropisomeric 3-(2-substituted aryl)quinazolin-4-ones and their stereochemical properties Reviewed
Tokitoh Takashi, Kobayashi Toshitake, Nakada Eisuke, Inoue Tohru, Yokoshima Satoshi, Takahashi Hideyo, Natsugari Hideaki
HETEROCYCLES Vol. 70 page： 93-+ 2006.12
Total synthesis of (+/-)-morphine Reviewed
Uchida Kenji, Yokoshima Satoshi, Kan Toshiyuki, Fukuyama Tohru
ORGANIC LETTERS Vol. 8 ( 23 ) page： 5311-5313 2006.11
Synthesis of biotinylated photoaffinity probes based on arylsulfonamide gamma-secretase inhibitors Reviewed
Fuwa Haruhiko, Hiromoto Kenichi, Takahashi Yasuko, Yokoshima Satoshi, Kan Toshiyuki, Fukuyama Tohru, Iwatsubo Takeshi, Tomita Taisuke, Natsugari Hideaki
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS Vol. 16 ( 16 ) page： 4184-4189 2006.8
Novel gamma-secretase inhibitors discovered by library screening of in-house synthetic natural product intermediates Reviewed
Takahashi Y, Fuwa H, Kaneko A, Sasaki M, Yokoshima S, Koizumi H, Takebe T, Kan T, Iwatsubo T, Tomita T, Natsugari H, Fukuyama T
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS Vol. 16 ( 14 ) page： 3813-3816 2006.7
Stereocontrolled total synthesis of (+)-vincristine Reviewed
Kuboyama T, Yokoshima S, Tokuyama H, Fukuyama T
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA Vol. 101 ( 33 ) page： 11966-11970 2004.8
A novel palladium-catalyzed coupling of thiol esters with 1-alkynes Reviewed
Tokuyama H, Miyazaki T, Yokoshima S, Fukuyama T
SYNLETT ( 10 ) page： 1512-1514 2003.8
Stereocontrolled total synthesis of (+)-vinblastine Reviewed
Yokoshima S, Ueda T, Kobayashi S, Sato A, Kuboyama T, Tokuyama H, Fukuyama T
PURE AND APPLIED CHEMISTRY Vol. 75 ( 1 ) page： 29-38 2003.1
Reduction of ethanethiol esters to aldehydes Reviewed
Tokuyama H, Yokoshima S, Lin SC, Li LP, Fukuyama T
SYNTHESIS-STUTTGART ( 8 ) page： 1121-1123 2002.6
Stereocontrolled total synthesis of (+)-vinblastine Reviewed
Yokoshima S, Ueda T, Kobayashi S, Sato A, Kuboyama T, Tokuyama H, Fukuyama T
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY Vol. 124 ( 10 ) page： 2137-2139 2002.3
A novel oxidative transformation of alpha-aminonitriles to amides Reviewed
Yokoshima S, Kubo T, Tokuyama H, Fukuyama T
CHEMISTRY LETTERS ( 2 ) page： 122-123 2002.2
Dogger Bank Itch revisited: isolation of (2-hydroxyethyl) dimethylsulfoxonium chloride as a cytotoxic constituent from the marine sponge Theonella aff. mirabilis Reviewed
Warabi K, Nakao Y, Matsunaga S, Fukuyama T, Kan T, Yokoshima S, Fusetani N
COMPARATIVE BIOCHEMISTRY AND PHYSIOLOGY B-BIOCHEMISTRY & MOLECULAR BIOLOGY Vol. 128 ( 1 ) page： 27-30 2001.1
Enantioselective total synthesis of (+)-gelsemine: Determination of its absolute configuration Reviewed
Yokoshima S, Tokuyama H, Fukuyama T
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION Vol. 39 ( 22 ) page： 4073-4075 2000
A novel ketone synthesis by a palladium-catalyzed reaction of thiol esters and organozinc reagents Reviewed
Tokuyama H, Yokoshima S, Yamashita T, Fukuyama T
TETRAHEDRON LETTERS Vol. 39 ( 20 ) page： 3189-3192 1998.5
Facile palladium-mediated conversion of ethanethiol esters to aldehydes and ketones Reviewed
Tokuyama H, Yokoshima S, Yamashita T, Lin SC, Li LP, Fukuyama T
JOURNAL OF THE BRAZILIAN CHEMICAL SOCIETY Vol. 9 ( 4 ) page： 381-387 1998
天然物の化学II 自然からの贈り物
上村大輔 他（ Role： Joint author）
東京化学同人 2018.7
天然有機化合物の全合成
井上将行 他（ Role： Sole author）
化学同人 2018.3
アルカロイドの科学
高山廣光 他（ Role： Sole author）
化学同人 2017.8
天然物の化学 ー魅力と展望ー
上村大輔 他（ Role： Joint author）
東京化学同人 2016.6
天然物合成で活躍した反応
菅敏幸、林雄二郎、長澤和夫、福山透、岡野健太郎、庄司満、高橋圭介、早川一郎、山口潤一郎、山下修治、横島聡、吉村文彦（ Role： Joint author）
化学同人 2011.10 （ ISBN:978-4-7598-1479-8 ）
天然物全合成の最新動向
北泰行 他（ Role： Sole author）
シーエムシー出版 2009.11
Grant number：23H02602 2023.4 - 2026.3
科学研究費助成事業 基盤研究(B)
横島 聡
Authorship：Principal investigator
Grant amount：\18720000 （ Direct Cost: \14400000 、 Indirect Cost：\4320000 ）
創薬分子基盤の確立を指向し、複数の環が組み合わさった三次元的に広がりのある骨格に、官能基や置換基が配置される構造の合成法開発を目的として、天然物の合成研究を実施する。複雑な構造をもつ分子の合成は情報学的な反応の集積のみでは実施することが困難であり、分子挙動の理解が必要不可欠である。実験を通して分子の構造・性質に関する情報を的確に得て、それらを繰り込んだ合成計画の立案、多面的な検討を経て、合成経路を確立する。
Development of monoclonal antibody targeting CHRNB2 to treat gastric cancer
Grant number：20H03750 2020.4 - 2024.3
Grants-in-Aid for Scientific Research Grant-in-Aid for Scientific Research (B)
Authorship：Coinvestigator(s)
多環式含窒素コア骨格と大環状構造を特徴とする海洋性中分子の合成研究
Grant number：18H04399 2018.4 - 2020.3
新学術領域研究(研究領域提案型)
横島 聡
Authorship：Principal investigator
Grant amount：\5200000 （ Direct Cost: \4000000 、 Indirect Cost：\1200000 ）
ハリクロニンAの合成研究：立体選択的アルキル化、閉環メタセシス、および分子内シクロプロパン化反応を鍵工程とした合成経路を用いて、大員環をもつアザビシクロ[3.3.1]ノナン骨格の構築を行い、さらなる検討に必要な十分量の基質の合成を行った。得られた化合物の第一級アルコール部位を酸化することでアルデヒドを得たのち、エナミンを経由して立体選択的にフェニルセレネニル基を導入した。過酸化水素を用いてセレノキシドへと酸化したところ、シン脱離が円滑に進行し、望みの幾何異性をもつ不飽和アルデヒドを得ることができた。本アルデヒドにアリルボロン酸エステルをさせたところ、高い立体選択性でアリル基の導入を行うことができ、天然物と同一の立体化学をもつ第二級アルコールを得た。導入したアリル基の末端オレフィン部位と、既に導入されていた窒素原子上の側鎖の末端オレフィン部位を閉環メタセシスにより連結し、2つ目の大員環を構築した。さらに脱保護、ホルミル基の導入、ケトンへの酸化を含む数工程で、ハリクロニンAへと導いた。デンサニンBの合成研究：不斉ディールス・アルダー反応、ジブロモシクロプロパンの開裂による環拡大反応、2-ニトロベンゼンスルホンアミド部位とアルコール部位との分子内置換反応を用いて、大員環をもつシクロヘプテノンを得た。シクロヘプテノン部位をあしがかりとしたピロリジン環の構築について検討を行ったところ、アゾメチンイリドの環化付加反応により、望みとするピロリジン環を構築可能であることが明らかとなった。すなわち上記シクロヘプテノンに対して、アセトニトリル中フッ化リチウム存在下、アゾメチンイリドの前駆体としてN-ベンジル-N-メトキシメチルトリメチルシリルメチルアミンを作用させ、加熱したところ、アゾメチンイリドの環化付加反応が進行し、ピロリジン環を含む三環性化合物を得ることに成功した。
令和元年度が最終年度であるため、記入しない。
令和元年度が最終年度であるため、記入しない。
Grant number：17H01523 2017.4 - 2022.3
科学研究費助成事業 基盤研究(A)
横島 聡
Authorship：Principal investigator
Grant amount：\41080000 （ Direct Cost: \31600000 、 Indirect Cost：\9480000 ）
ダフニフィラムアルカロイドの合成研究：ダフニフィラムアルカロイドに広く見られる共通構造である、不斉第四級炭素、連続する２つの不斉中心、およびそれらに隣接した四置換二重結合を含む三環性骨格をもつ天然物の合成研究を行った。Diels-Alder反応を用いて環構造の構築を行い、環拡大反応を適用することで、必要な置換基を備えた7員環化合物を得た。さらにその中間体から、エキソメチレン部位の構築、ビニル基の導入を行い、電子環状反応に続く分子内付加反応を実施し、目的とする構造を得ることに成功した。更に窒素原子を含む環構造の構築にも成功した。以上の成果を論文として発表した。リコポジウムアルカロイドの合成研究：これまでにケトン部位およびヒドロキシアミン部位の両方をあわせ持つ化合物からアミナール構造が構築可能であることが見いだされていたが、この知見を発展させ、直接的にアミナール構造をもつ天然物の合成経路を確立することに成功した。またアミナール形成時に還元条件を適用することで、ピロリジン環の構築にも成功し、ピロリジン環を含む天然物の合成経路の確立にも成功した。その他に、閉環メタセシス反応またはカスケードHeck反応を駆使することで、天然物の環状構造を構築する検討を行った。それらの合成において、基質の立体化学が反応の結果に大きな影響を与えることを見出し、適切な立体化学を備えた化合物を用いることで、効率的に目的とする構造を有する化合物を得ることに成功した。
令和3年度が最終年度であるため、記入しない。
令和3年度が最終年度であるため、記入しない。
多環式含窒素コア骨格と大環状構造を特徴とする海洋性中分子の合成研究
Grant number：16H01141 2016.4 - 2018.3
新学術領域研究(研究領域提案型)
横島 聡
Authorship：Principal investigator
Grant amount：\5720000 （ Direct Cost: \4400000 、 Indirect Cost：\1320000 ）
韓国近海のホヤより単離・構造決定されたハリクロニンAの合成研究を行った。昨年度までに合成法を確立していたビシクロ骨格を含む化合物を出発物質とした検討を行っていたが、さらなる官能基変換が困難であることが明らかとなった。そこでビシクロ骨格構築の前に、あらかじめ官能基変換を行う合成経路の検討を行った。その結果、ビシクロ骨格およびその後の変換に必要な官能基をもつ化合物を得ることに成功した。また上記の検討と並行して、酸化的脱芳香環化に続く分子内環化付加反応を基軸とした合成経路について検討を行った。フェノール性水酸基を足がかりとしてベンゼン環上に必要な置換基を導入し、分子内環化付加反応の前駆体を合成した。酸化的脱芳香環化は通常用いられる条件にて円滑に進行し、さらに加熱を行うことで分子内環化付加反応が進行することが明らかとなった。その結果、第四級炭素およびその後の変換に必要となる官能基を含む部分骨格の構築に成功した。デンサニンBの合成研究については以下に述べる知見を得るに至った。不斉ディールスアルダー反応、ジブロモシクロプロパンの開裂による環拡大反応、2-ニトロベンゼンスルホンアミド部位の分子内置換反応を用いて構築した二環性骨格の立体的特性を利用した官能基の選択的な導入について検討を行った。その結果、エノンに対する共役付加が架橋鎖を避ける側から立体選択的に進行することを見出し、第四級炭素の構築に成功した。
29年度が最終年度であるため、記入しない。
29年度が最終年度であるため、記入しない。
基盤創薬学概論
2020
化学基礎II
2020
化学基礎II
2019
基盤創薬学概論
2019
農学セミナー
2019
生理活性物質化学
2019
先端有機化学
2019
創薬精密科学
2019
