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公开(公告)号:US5770767A
公开(公告)日:1998-06-23
申请号:US593940
申请日:1996-01-30
申请人: Nobushige Itaya , Ryuhei Wakita , Asako Kubo , Mikio Sasaki , Takashi Namba , Yusuke Yukimoto
发明人: Nobushige Itaya , Ryuhei Wakita , Asako Kubo , Mikio Sasaki , Takashi Namba , Yusuke Yukimoto
IPC分类号: C07C51/377 , C07C61/15 , C07C61/04
CPC分类号: C07C61/15 , C07C51/377
摘要: A process for producing a 2-fluorocyclopropane-carboxylic acid of formula �I! ##STR1## by reducing a 2-halo-2-fluorocyclopropanecarboxylic acid of formula �II! ##STR2## the reduction being carried out by developing a Raney nickel alloy in the presence of the 2-halo-2-fluorocyclo-propanecarboxylic acid of formula �II!, or by contacting the 2-halo-2-fluorocyclopropanecarboxylic acid of formula �II! with hydrogen in an aqueous solvent using a Raney nickel catalyst.
摘要翻译: 通过还原式[II]的2-卤代-2-氟环丙烷羧酸[II],制备式[I]的2-氟环丙烷 - 羧酸的方法通过将式[II]的2-卤代-2-氟环丙烷羧酸还原为 在式[II]的2-卤代-2-氟代环丙烷羧酸存在下研磨阮内镍合金,或者通过使式[Ⅱ]的2-卤代-2-氟环丙烷羧酸与氢在水溶剂中接触,使用 阮内镍催化剂。
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公开(公告)号:US5693814A
公开(公告)日:1997-12-02
申请号:US303812
申请日:1994-09-12
申请人: Youichi Kimura , Katsuhiro Kawakami , Norimasa Mikata , Keiji Uchiyama , Tazuo Uemura , Yusuke Yukimoto
发明人: Youichi Kimura , Katsuhiro Kawakami , Norimasa Mikata , Keiji Uchiyama , Tazuo Uemura , Yusuke Yukimoto
IPC分类号: A61K9/00 , C07D401/04 , A61K31/47 , A61K31/4747 , A61P31/04 , A61P35/04 , C07B63/00 , C07D215/56 , C07D221/00 , C07D401/10 , C07D403/04 , C07D471/04 , C07D215/18 , C07D215/38
CPC分类号: C07D401/04
摘要: A method for selectively obtaining any one of an anhydrate, a 1/2 hydrate, a 1 hydrate, and a 3/2 hydrate of 7-�(7-(S)-amino-5-azaspiro�2.4!heptan-5-yl!-8-chloro-6-fluoro-1-�(1R,2S)-2-fluorocyclopropyl!-4-oxo-1,4-dihydroquinoline-3-carboxylic acid is disclosed, comprising treating the compound in an aqueous solvent or water or recrystallizing the compound from an aqueous solvent or water.
摘要翻译: 一种选择性地获得7 - [(7-(S) - (C 1 -C 6)烯的水合物,+ E,F 1/2 + EE水合物,1水合物和+ 氨基-5-氮杂螺[2.4]庚-5-基] -8-氯-6-氟-1 - [(1R,2S)-2-氟环丙基] -4-氧代-1,4-二氢喹啉-3-羧酸 酸,包括在水性溶剂或水中处理化合物或者从水性溶剂或水中重结晶化合物。
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公开(公告)号:US5780669A
公开(公告)日:1998-07-14
申请号:US592402
申请日:1996-02-01
申请人: Toshifumi Akiba , Takanobu Ikeya , Hirofumi Kawanishi , Yusuke Yukimoto , Shinji Kamihara , Tsutomu Ebata
发明人: Toshifumi Akiba , Takanobu Ikeya , Hirofumi Kawanishi , Yusuke Yukimoto , Shinji Kamihara , Tsutomu Ebata
IPC分类号: C07C51/377 , C07C67/317 , C07C69/74
CPC分类号: C07C51/377 , C07C67/317
摘要: A compound represented by the following formula (1) or (3): ##STR1## is subjected to a catalytic hydrogenolysis reaction in the presence of a base and thus a compound represented by the following formula (2): ##STR2## wherein R represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms and X represents a chlorine atom or a bromine atom; is easily produced. This compound is usable as an intermediate for the preparation of drugs.
摘要翻译: PCT No.PCT / JP94 / 01280 Sec。 371日期:1996年2月1日 102(e)日期1996年2月1日PCT 1994年8月3日PCT PCT。 出版物WO95 / 04712 日期:1995年2月16日由下式(1)或(3)表示的化合物:在碱的存在下进行催化氢解反应,因此代表的化合物 (2)其中R表示氢原子或碳原子数1〜4的烷基,X表示氯原子或溴原子, 很容易生产。 该化合物可用作制备药物的中间体。
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