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公开(公告)号:US6013653A
公开(公告)日:2000-01-11
申请号:US43121
申请日:1998-04-21
申请人: Kooji Kagara , Nobutaka Kawai , Takashi Nakamura , Shigeru Ieda , Koji Machiya , Atsushi Ohigashi
发明人: Kooji Kagara , Nobutaka Kawai , Takashi Nakamura , Shigeru Ieda , Koji Machiya , Atsushi Ohigashi
IPC分类号: C07D471/04 , A61K31/44 , A61K31/435 , C07D221/06
CPC分类号: C07D471/04 , Y02P20/55
摘要: A process for producing pyridiondole derivatives represented by general formula (III) or their salts (wherein R.sup.1 represents hydrogen, lower alkyl or lower alkenyl; R.sup.2 represents hydrogen, lower alkyl or halogeno; and R.sup.3 represents optionally substituted imidazolyl), which comprises reacting a compound represented by general formula (I) or its salt (wherein R.sup.1 and R.sup.2 are each as defined above) with a compound represented by general formula (II) or its salt (wherein R.sup.3.sub.a represents optionally substituted imidazolyl having an imino protecting group; and X represents halogeno), followed by a reaction for eliminating the imino protecting group); and a process for producing optically active pyridoindole derivatives represented by general formula (IV) or their salts: which comprises reacting a racemic mixture of the pyridoindole derivative represent by formula (III) or its salt with (1R)-(-)-10-camphorsulfonic acid.
摘要翻译: PCT No.PCT / JP96 / 02692 Sec。 371日期:1998年4月21日 102(e)1998年4月21日PCT PCT 1996年9月18日PCT公布。 出版物WO97 / 11074 日本1997年3月27日制备通式(III)表示的吡啶并衍生物或其盐(其中R1表示氢,低级烷基或低级烯基; R2表示氢,低级烷基或卤代; R3代表任意取代的咪唑基)的方法, 其包括使通式(I)表示的化合物或其盐(其中R 1和R 2各自如上定义)与通式(II)表示的化合物或其盐(其中R 3a表示任选取代的具有亚氨基保护的咪唑基) 基团,X表示卤代),然后进行反应,除去亚氨基保护基)。 以及由通式(IV)表示的光学活性吡啶并吲哚衍生物或其盐的方法,其包括使式(III)表示的吡啶并吲哚衍生物的外消旋混合物或其盐与(1R) - ( - ) - 樟脑磺酸。
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公开(公告)号:US5523410A
公开(公告)日:1996-06-04
申请号:US360683
申请日:1995-01-03
申请人: Kooji Kagara , Nobutaka Kawai , Koji Machiya , Tetsuo Furutera , Takashi Nakamura , Hiroki Omori
发明人: Kooji Kagara , Nobutaka Kawai , Koji Machiya , Tetsuo Furutera , Takashi Nakamura , Hiroki Omori
IPC分类号: C07D233/54 , C07D233/64 , C07D413/12
CPC分类号: C07D233/64 , C07D233/54 , Y02P20/55
摘要: The present invention relates to synthetic intermediates useful for preparing amino acid derivatives possessing renin-inhibitory activity, and to processes for preparing the amino acid derivatives using the synthetic intermediates.
摘要翻译: PCT No.PCT / JP93 / 00885 Sec。 371日期1995年1月3日 102(e)日期1995年1月3日PCT提交1993年6月28日PCT公布。 公开号WO94 / 01409 日本1994年1月20日。本发明涉及可用于制备具有肾素抑制活性的氨基酸衍生物的合成中间体,以及使用合成中间体制备氨基酸衍生物的方法。
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公开(公告)号:US5254733A
公开(公告)日:1993-10-19
申请号:US775456
申请日:1991-10-15
申请人: Kooji Kagara , Nobutaka Kawai , Koji Machiya , Kiyoaki Takasuka
发明人: Kooji Kagara , Nobutaka Kawai , Koji Machiya , Kiyoaki Takasuka
IPC分类号: C07C249/06 , C07C251/40 , C07C233/09
CPC分类号: C07C249/06
摘要: The present invention relates to a process for producing (.+-.)-(E)-4-ethyl-2-[E-hydroxyimino]-5-nitro-3-hexenamide.
摘要翻译: 本发明涉及一种生产(+/-) - (E)-4-乙基-2- [E-羟基亚氨基] -5-硝基-3-己烯酰胺的方法。
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公开(公告)号:US06455726B2
公开(公告)日:2002-09-24
申请号:US09782291
申请日:2001-02-14
IPC分类号: C07C22900
CPC分类号: C07C227/06 , C07C229/38 , C07C229/34
摘要: A compound of the following formula (II) and a process for preparing of the compound of the following formula (I) its preparation wherein R1 is carboxy or protected carboxy; R2 is lower alkoxy or higher alkoxy; A1 is a divalent aromatic ring, a divalent heterocyclic group or a divalent cyclo(lower)alkane; and A2 is a divalent aromatic ring, a divalent heterocyclic group or a divalent cyclo(lower)alkane, or a salt thereof. The process comprises, reacting a compound of the formula (III): wherein R1, R2, A1 and A2 are each as defined above or a salt thereof, with an acid ammonium salt to give a compound of the formula (II).
摘要翻译: 下式(II)的化合物及其制备方法,其中R1为羧基或被保护的羧基; R2为低级烷氧基或高级烷氧基; A1为二价芳环,二价杂环 基团或二价环(低级)烷烃; 和A 2是二价芳环,二价杂环基或二价环(低级)烷烃或其盐。 该方法包括使式(III)化合物:其中R1,R2,A1和A2各自如上定义,或其盐与酸性铵盐反应,得到式(II)化合物。
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公开(公告)号:US06344559B1
公开(公告)日:2002-02-05
申请号:US09380609
申请日:1999-10-13
IPC分类号: C07D23996
CPC分类号: C07D239/96
摘要: This invention provides an industrially useful process for producing a quinazoline derivative (I) of the general formula: [wherein R1 is hydrogen or halogen; R2 is carboxy or protected carboxy; A is lower alkylene] or its salt on a commercial scale which comprises reacting a compound of the general formula: [wherein R1 is hydrogen or halogen] or its salt with a silylating agent and then with a compound of the general formula: Cl—A—R2 (III) [wherein R2 is carboxy or protected carboxy; A is lower alkylene] or its salt, optionally followed by desilylation.
摘要翻译: 本发明提供了一种工业上有用的制备具有以下通式的喹唑啉衍生物(I)的方法:其中R 1是氢或卤素; R2是羧基或被保护的羧基; A是低级亚烷基]或其盐,其包括使通式为[其中R 1为氢或卤素]的化合物或其盐与甲硅烷基化试剂反应,然后与下列通式的化合物反应:其中R 2 是羧基或被保护的羧基; A是低级亚烷基]或其盐,任选地随后脱甲硅烷基化。
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公开(公告)号:US06291680B1
公开(公告)日:2001-09-18
申请号:US09446359
申请日:1999-12-20
IPC分类号: C07D261106
CPC分类号: C07C227/06 , C07C229/38 , C07C229/34
摘要: A compound of formula (1) or a salt thereof: wherein R1 is a carboxy or a protected carboxy; R2 is a lower alkoxy or a higher alkoxy; A1 is a divalent aromatic ring, a divalent heterocyclic group or a divalent cyclo(lower)alkane; and A2 a divalent aromatic ring, a divalent heterocyclic group or a divalent cyclo(lower)alkane; is prepared by reacting a compound of formula (III) or a salt thereof with acid ammonium salt: wherein R1, R2, A1 and A2 are each as defined above; to give a compound of formula (II) or a salt thereof which is further reacted with a salt of hydroxylamine: wherein R1, R2, A1 and A2 are each as defined above.
摘要翻译: 式(1)的化合物或其盐:其中R1是羧基或被保护的羧基; R2是低级烷氧基或高级烷氧基; A1是二价芳环,二价杂环基或二价环(低级)烷烃; 和A2为二价芳环,二价杂环基或二价环(低级)烷烃; 通过使式(III)的化合物或其盐与酸性铵盐反应制备:其中R1,R2,A1和A2各自如上所定义; 得到与羟胺盐进一步反应的式(II)化合物或其盐:其中R1,R2,A1和A2各自如上所定义。
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公开(公告)号:US06355800B1
公开(公告)日:2002-03-12
申请号:US09509812
申请日:2000-04-06
申请人: Kooji Kagara , Norio Hashimoto , Atsushi Kanda , Yukihisa Baba , Tetsuo Furutera
发明人: Kooji Kagara , Norio Hashimoto , Atsushi Kanda , Yukihisa Baba , Tetsuo Furutera
IPC分类号: C07D29532
CPC分类号: C07D295/32
摘要: A new industrial process excellent in yield and purity for preparing a compound of the formula: or a salt thereof in a less number of steps with a synthetic pathway without proceeding via nitroso compounds, wherein R1 is lower aryl, ar(lower)alkoxy or heterocyclic group, each of which may be substituted with halogen, and R2 is cyclo(lower)alkyl, aryl or ar(lower)alkyl, each of which may be substituted with halogen.
摘要翻译: 一种新的工业方法,其具有优良的产率和纯度,用于通过合成途径制备下式化合物或其盐在较少数量的步骤中,而不经由亚硝基化合物进行,其中R 1为低级芳基,芳(低级)烷氧基或杂环 基团,其各自可以被卤素取代,并且R 2是环(低级)烷基,芳基或芳(低级)烷基,其各自可以被卤素取代。
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