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Shimomura Naoyuki, Sasho Manabu, Kayano Akio, Yoshizawa Kazuhiro, Tsujii Masahiko, Kuroda Hiroshi, Furukawa Ken: (Ja) 環状ベンズアミジン誘導体の製造方法, (En) Processes for producing cyclic benzamidine derivative. Eisai, Shimomura Naoyuki, Sasho Manabu, Kayano Akio, Yoshizawa Kazuhiro, Tsujii Masahiko, Kuroda Hiroshi, Furukawa Ken, SHIMIZU Hatsushi, September 16, 2004: WO/2004/078721 (13 worldwide citation)

(EN) A process for producing a fluorinated cyclic benzamidine derivative (A) or salt thereof, characterized by comprising the step of reacting a specific novel compound with ammonia or an imide; a process for producing a morpholine-substituted phenacyl derivative (B) or salt thereof, characterized b ...


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Shimomura Naoyuki, Sato Nobuaki, Kaneko Toshihiko, Takaishi Mamoru, Wakasugi Kazunori, Yoshikawa Seiji, Nishikawa Yoshihiro, Nakamura Taiju, Hukuyama Tohoru: (Ja) シンナミド誘導体の製造方法, (En) Process for production of cinnamamide derivative. Eisai R & D Management, Shimomura Naoyuki, Sato Nobuaki, Kaneko Toshihiko, Takaishi Mamoru, Wakasugi Kazunori, Yoshikawa Seiji, Nishikawa Yoshihiro, Nakamura Taiju, Hukuyama Tohoru, ASAMURA Kiyoshi, May 24, 2007: WO/2007/058305 (10 worldwide citation)

(EN) A compound (8) represented by the formula: (8) [wherein R1 represents a 6- to 14-membered aromatic hydrocarbon ring group which may have a substituent; and n represents 0 to 2] can be produced with good efficiency by reacting a compound (1) represented by the formula: (3) [wherein R1 and n are ...


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Shimomura Naoyuki, Kamada Atsushi, Miyazawa Mamoru, Ito Koichi: (Ja) ピペリジン環を有するインドール誘導体の製造方法, (En) Method for producing indole derivative having piperidine ring. Eisai R & D Management, Shimomura Naoyuki, Kamada Atsushi, Miyazawa Mamoru, Ito Koichi, ASAMURA Kiyoshi, November 16, 2006: WO/2006/121106 (2 worldwide citation)

(EN) It is possible to commercially advantageously produce 1-{1-[2-(7-methoxy-2,2-dimethyl-4-oxochroman-8-yl)ethyl] piperidin-4-yl}-N-methyl-1H-indole-6-carboxamide by coupling (7-methoxy-2,2-dimethyl-4-oxochroman-8-yl)acetaldehyde, which is obtained by oxidizing 8-(2-hydroxyethyl)-7-metho ...


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Negi Shigeto, Shimizu Toshikazu, Kuroda Hiroshi, Shimomura Naoyuki, Sasho Manabu, Hoshino Yorihisa, Kubota Manabu: (Ja) ピラゾール縮合環誘導体の製造方法, (En) Process for production of pyrazole-fused ring derivatives. Eisai R & D Management, Negi Shigeto, Shimizu Toshikazu, Kuroda Hiroshi, Shimomura Naoyuki, Sasho Manabu, Hoshino Yorihisa, Kubota Manabu, INAMI Minoru, October 27, 2005: WO/2005/100354

(EN) The invention aim at finding intermediates useful in the synthesis of pyrazole-fused ring derivatives (such as 7-phenylpyrazolo[1,5-a]pyridine derivatives) and a process for the production thereof. A process for the production of compounds represented by the general formula (II), salts thereof, ...


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Shimomura Naoyuki, Yoshikawa Seiji, Hisatake Yoshihiko, Imai Akio: (Ja) シンナミド誘導体のワンポット製造方法, (En) One-pot production process for cinnamide derivative. Eisai R & D Management, Shimomura Naoyuki, Yoshikawa Seiji, Hisatake Yoshihiko, Imai Akio, ASAMURA Kiyoshi, November 20, 2008: WO/2008/140111

(EN) A compound represented by the formula (1) below or a pharmaceutically acceptable salt thereof is able to be produced in one pot by reacting a compound represented by the formula (2) below with 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzaldehyde in the presence of a base, and if necessary, by re ...


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Ikuta Hironori, Shimomura Naoyuki, Akamatsu Hiroshi, Matsuo Kimihiro: (Ja) n-(3-クロロ-1h-インドール-7-イル)-4-スルファモイルベンゼンスルホンアミドの製造方法, (En) Process for producing n-(3-chloro-1h-indol-7-yl)-4-sulfamoylbenzenesulfonamide. Eisai R & D Management, Ikuta Hironori, Shimomura Naoyuki, Akamatsu Hiroshi, Matsuo Kimihiro, ASAMURA Kiyoshi, May 26, 2006: WO/2006/054491

(EN) 7-Nitroindole is chlorinated with N-chlorosuccinimide in a hydrous solvent to produce 3-chloro-7-nitroindole (II). The compound (II) is reduced to obtain 3-chloro-7-aminoindole. This compound or its hydrochloride is reacted in the presence of a base with 4-sulfamoylbenzenesulfonyl chloride synt ...


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Sato Keizo, Nara Kazumasa, Shimomura Naoyuki: (Ja) ピラゾール縮合環誘導体の製造方法, (En) Method for producing pyrazole fused ring derivative. Eisai R & D Management, Sato Keizo, Nara Kazumasa, Shimomura Naoyuki, INAMI Minoru, April 23, 2009: WO/2009/051210

(EN) Disclosed is a commercially advantageous method for producing a pyrazole fused ring derivative (such as a 7-phenylpyrazolo[1,5-a]pyridine derivative). Specifically disclosed is a method for producing a compound (I) represented by the formula (I) below or a salt thereof, which comprises a step A ...