Japanese Society for Process Chemistry

 
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2011 Hayato Ishikawa, Masakazu Honma, Yujiro Hayashi* (Tokyo University of Science, Japan) One-Pot High-Yielding Synthesis of the DPP4-Selective Inhibitor ABT-341 by a Four-Component Coupling Mediated by a Diphenylprolinol Silyl Ether Ryoki Orii*, Takashi Kikuchi (Astellas Pharma Inc., Japan) Development of a practical synthesis for HDAC Inhibitor AS1623879-CL Daisuke Takahashi* (AJINOMOTO Co., Inc. Japan) Development of a Novel Liquid-Phase Peptide Synthesis (LPPS) on Anchors Bearing a Long Aliphatic Chain: AJI-PHASETM Masahiro Egi1), Koji Sugiyma1)*, Moriaki Saneto1), Ryosuke Hanada1), Katsuya Kato2), Shuji Akai1) [(1)University of Shizuoka, Japan, (2)National Institute of Advanced Industrial Science and Techology, Japan] Asymmetric Synthesis of Allyl Esters via Vanadium-Lipase Combo Catalyzed Dynamic Kinetic Resolution.
JSPC Award for Excellence

Recognizes notable contributions to process chemistry.
The awardees will be selected as a research group from the general presentation at the summer symposium.
The award consists of a testimonial shield and the awardee should represent their research works at the appropriate symposium.

Awardees
2015

1P-01
Kaori Ando*, Takahisa Kobayashi, Nariaki Uchida
(Department of Chemistry and Biomolecular Science, Faculty of Engineering, Gifu University)
"Highly Practical New Methylenation Reagent for Aldehydes and Ketones"

1P-36
Yuji Takahama*, Kazuhiro Takeguchi, Kazuyoshi Obitsu, Norihiro Ueda, Ryoki Orii, Atsushi Ohigashi, Shigeru Ieda, Minoru Okada
iProcess Chemistry Laboratories, Astellas Pharma Inc.j
"Root Cause Analysis of Uncontrollable Polymorph -Inhibition of a Trace Amount of Impurity in Selective ALK Inhibitor ASP3026-"
2014

Tomohide Okada*1,Tomotake Asawa1,Yukihiro Sugiyama2,Masyuki Kirihara3,Toshiaki lwai3, Yoshikazu Kimura4
(1R&D Department of Chemicals, Nippon Light Metal Company Ltd.
2Market Development Department, Nippon Light Metal Company Ltd.
3Department of Materials and Life Science, Shizuoka Institute of Science and Technology
4Research and Development Department, Iharanikkei Chemical lndustry Co. Ltd.)

Practical Oxidation Reaction of Alcohols with Sodium Hypochlorite Pentahydrate(NaClO-5H2O)Crystals

Masatoshi Yamada1*, Takahiro Konishi1, Masayuki Yamashita1, Mitsutaka Goto2, Takashi Nihei1, Keiichirou Nakaoka1, Tetsuhiro Yamamoto1, Mitsuhisa Yamano1
(1Chemical Deveropment Laboratories, CMC Center, Takeda Pharmaceutical Company Limited,
2Chemical Technology Department, Pharmaceutical Production Division)

Development of manufacturing process for fasiglifam via asymmetric hydrogenation with trace ruthenium catalyst

Hiroyoshi Morimoto*, Risa Fujiwara, Yuhei Shimizu, Kazuhiro Morisaki, Takashi Ohshima
(Graduate School of Pharmaceutical Sciences, Kyushu University)

Lanthanum(III) Triflate-Catalyzed Direct Amidation of Esters

2013

Takashi Naka*, Kenichi Toyama, Hiroki Ozawa
(Process Chemistry Research Laboratories, CMC Division, Mitsubishi Tanabe Pharma Corporation)

Process Safety Evaluation and Scale-up of a Lactum Reduction with NaBH4 and TFA

Naohiro Fukuda*, Yasuhiro Sawai, Takeshi Yamasaki, Yukio Minato, Takashi Sagawa, Atsushi Inagaki, Shinichi Urayama, Tomomi Ikemoto
(Chemical Development Laboratories, CMC Center, Takeda Pharmaceutical Company Limited)

Imide-Catalyzed Oxidation of Sulfides with NaOCl and the Application to a Drug Candidate

Atsuki Kato*, Taito Koyama, Takeshi Oriyama
Fucalty of Science, Ibaraki University

One-Step Conversion of Silyl Ethers to Esters by Using BF3/THP

2012
Atsushi Akao*, Yusuke Miyashita, Hiroshi Oe, Yuki Kosaka, Jun Nishijima and Masaaki Hori
(API Research, Eisai Product Creation Systems)

Reaction Analyses / Monitorings by LC-MS; Toward Process Understandings
Masayuki Utsugi*, Hiroki Ozawa, Masanori Hatsuda
(Process Chemistry Research Laboratories, CMC Division, Mitsubishi Tanabe Pharma Corporation)

Scale-up Studies on Synthesis of Benzonitrile Derivarive via Pd-Catalyzed Cyanation
Shun Hirasawa*, Kazuyoshi Obitsu, Kazuhiro Takeguchi, Ryoki Orii, Shigeru Ieda, Minoru Okada
(Process Chemistry Laboratories, Astellas Pharma Inc.)

Polymorphic Control of Novel ALK Inhibitor ASP3026 via Solvent-Mediated Polymorphic Transformation

Tsubasa Sakamoto*, Keiji Mori, Takahiko Akiyama
(Department of Chemistry, Faculty of Science, Gakushuin University)

Phosphoric Acid Catalyzed Enantioselective Transfer Deutration of Ketimines by Use of Deutrated Benzothiazoline

2011

Hayato Ishikawa, Masakazu Honma, Yujiro Hayashi*
(Tokyo University of Science, Japan)

One-Pot High-Yielding Synthesis of the DPP4-Selective Inhibitor ABT-341 by a Four-Component Coupling Mediated by a Diphenylprolinol Silyl Ether

Ryoki Orii*, Takashi Kikuchi
(Astellas Pharma Inc., Japan)

Development of a practical synthesis for HDAC Inhibitor AS1623879-CL

Daisuke Takahashi*
(AJINOMOTO Co., Inc. Japan)

Development of a Novel Liquid-Phase Peptide Synthesis (LPPS) on Anchors Bearing a Long Aliphatic Chain: AJI-PHASETM

Masahiro Egi1), Koji Sugiyma1)*, Moriaki Saneto1), Ryosuke Hanada1), Katsuya Kato2), Shuji Akai1)
[(1)University of Shizuoka, Japan,(2)National Institute of Advanced Industrial Science and Techology, Japan]

Asymmetric Synthesis of Allyl Esters via Vanadium-Lipase Combo Catalyzed Dynamic Kinetic Resolution.

2010

Shunsuke Fukuya*, Michiharu Handa, Katsuya Sakata, Hiroyuki Kotajima, Motoi Otani
(Onda Plant, Technical Deveropment Division, Nissan Chemical Industries, Ltd., Japan)

Process deveropment of AZADO-catalyzed oxidation - Experimental demonstration by pirot scale production -

Hirofumi Maeda*, Akio Fujii, Masaru Mitsuda
(Frontier Biochemical& Medical Research Labratories, Kaneka Corporation, Japan)

Deveropment of Novel Phosphoramidite Monomer for Oligo RNA Synthesis

Yutaka Saga*, Rie Motoki, Sae Makino, Yohei Shimizu, Motomu Kanai, Masakatsu Shibasaki
(Graduate School of Pharmaceutical Sciences, The University of Tokyo, Japan)

Catalytic Asymmetric Synthesis of R207910
2009

Shinpei Iida, Ryosuke Ohmura, Hideo Togo*
(Graduate School of Science, Chiba University, Japan)

Direct Oxidative Conversion of Alcohols, Amines, and Alkyl halides into Nitriles with Molecular Iodine and 1,3-Diiodo-5,5-dimethylhydantoin in aq. Ammonia.

Kaichiro Koyama*, Hitoshi Shimizu, Shinichi Ebihara
(synthetic Technology Research Dept., Chugai Pharmaceutical & Co., Ltd., Japan)

Optimization of drying process in scale-up manufacturing for Erythromycin A derivative.

Osamu Ogata*, Yasunori Ino, Wataru Kuriyama, Takaji Matsumoto
(Corporate research & Development Division, Takasago International Corporation, Japan)

An Efficient Synthesis of Chiral Alcohols via Catalytic Hydrogen Reduction of Esters.
Hiromichi Fujioka, Kento Senami*, Ozora Kubo, Yutaka Minamitsuji, Tomohiro Maegawa
(Graduate School of Pharmaceutical Sciences, Osaka University, Japan)

Development of very mild and highly selective deprotection method of methylene acetals.
2008
Arata Yanagisawa*, Koichiro Nishimura ,Tetsuya Nezu, Kyoji Ando, Ayako Maki, Eiichiro Imai, Shin-ichiro Mohri
(Kyowa Hakko Kogyo, Japan)

A Practical Synthesis of the PDE4 inhibitor KW-4490.
Takashi Inaba*, Masahiro Tanaka, Minoru Ubukata, Takafumi Matsuo, Katsutaka Yasue, Katsuya Matsumoto, Yasuyuki Kajimoto, Takashi Ogo
(Japan Tobacco Inc.,Japan)

An Efficient Synthesis of the PKCb Inhibitor JTT-010 Using a Novel Cyclopropane Ring-Opening Reaction with Indole
Takashi Ohshima*, Takanori Iwasaki, Yusuke Maegawa, Yukiko Hayashi, Kazushi Mashima
(Osaka University, Japan)

Development of Protecting Group Free Catalytic O-Selective Acylation of Aminoalcohols
Kiwon Han*, Yoon Kyung Choi, Cheolwoo Kim, Jaiwook Park, Mahn-Joo Kim
(POSTECH, Korea)

Dynamic Kinetic Resolution of Primary Amines by Lipase-Palladium Cocatalysis
2007
Tetsuya Ikemoto, Yosuke Watanabe, Junichi Tomokawa, Takehiko Kawakami, Yasuo Uekita, and Isao Kurimoto
(Sumitomo Chemical Co.)

Process development of a key building block for anti-AIDS drugs by proline catalyzed enantioselective direct cross aldol reaction
Hideo Nagashima, Hidehiro Sasakuma, Nariaki Harada, Hironori Tsutsumi, and Yukihiro Motoyama (Kyushu Univ.)
Development of practical and scalable synthesis of triruthenium cluster catalyst and amide-selective silane reduction
Katsuo Oda, Toshiaki Masui, Hideo Nogusa, and Takemasa Hida
(Shionogi)

Development of process route for the new antiarthritic drug S-2474
2006
Ariyoshi Kubota, Koji Mukai, Shunsuke Goto, and Hironobu Yasuda
(Astellas Pharma)

Interesting characteristics and their control of polymorphs of bradykinin antagonist FR173657
Yumiko Okada, Shohei Yasuda, Jun Irie, Masaaki Takahashi, and Hitoshi Yamaguchi
(Meiji Seika)

Manufacturing process development of tricyclic triazolobenzazepine derivative
Yoshiharu Iwabuchi, Masatoshi Shibuya, Masaki Tomizawa, Takamune Hattori, and Takahisa Satoh (Tohoku Univ.)

Development of 1-methyl-AZADO: a highly efficient organocatalyst for oxidation of alcohols
2005
Shintaro Kanazawa and Ichiro Araya
(Kyorin)

Practical process developments of KRP-103 for treatment of urinary incontinence
Masahiro Nagase, Mitsuhiro Kurita, Takemi Tanokura, Motoki Shimizu, Yoshiaki Kato, Kunio Tamura, Hirohito Shimizu, and Masahiro Kato
(Chugai)

Process development of BO-653 for large scale production
Satomi Niwayama
(Texas Tech Univ., USA)

Practical monohydrolysis of symmetric diesters
Shuji Akai, Kouichi Tanimoto, Yukiko Kanao, Sohei Omura, and Yasuyuki Kita
(Osaka Univ.)

Lipase-catalyzed domino-type asymmetric construction of carbon frameworks: One-step synthesis of optically active polysubstituted isoxazolidines
2004
Ryohei Nagase, Naoki Manta, Tomonori Misaki, and Yoo Tanabe
(Kwansei Gakuin Univ.)

Makoto Sunagawa and Akira Sasaki (Sumitomo Pharmaceutical Co.) Practical synthesis of 1b-methylcarbapenem utilizing a new dehydration Ti-Dieckmann condensation
Yuuichi Katou, Tsutomu Sugawara, and Kazumi Okada
(Nippon Kasei)

Resolution technology of racemic mixtures using distillation technique in industrial scale
Takahiro Okachi and Katsuhiko Fujimoto
(Sankyo)

Practical promotion system for carbonyl-ene reactions styrenes with paraformaldehyde - The combined use of boron trifluoride and molecular sieves
2003
Shunsuke Goto, Hiroyuki Tsuboi, Atsuo Yamanaka, Kouji Mukai, and Kooji Kagara
(Fujisawa)

Process development of FK664: A potent cardiotonic agent
Mikio Kabaki and Haruo Koike
(Shionogi)

Process development of gastrointestinal ulser therapeutic agent S-0509
Takashi Ikawa, Hironao Sajiki, and Kosaku Hirota
(Gifu Pharmaceutical Univ.)

Environmental friendly mono-alkylation of aromatic amine derivatives
2002
Masaya Ikunaka, Yoshito Fujima, Toru Inoue, and Keisuke Matsuyama (Nagase) Shiro Kato, Hiroshi Harada, and Akihito Fujii
(Dainippon)

Synthesis of (R)-3-(2-aminopropyl)-7-benzyloxyindole, a key intermediate of antidiabetic AJ-9677, via optical resolution
Yuusaku Yokoyama, Hidemasa Hikawa, Masaharu Mitsuhashi, Yasuhiro Hiroki, and Yasuoki Murakami (Toho Univ.)

Synthesis without protection: Total synthesis of optically active clavicipitic acids utilizing a reaction of free amino acid
Youichi Matsumoto, Takeshi Murakami, and Yuuki Takuma
(Mitsubishi Chemical Corporation)

Study on the preparation of a chiral aminofuranone derivatives for antirheumatic agents
The Japanese Society for Process Chemistry