首页> 外国专利> PROCESS FOR THE PREPARATION OF a-(OXIMINO)- a-(1-AZABICYCLO 2.2.2 OCT- 3-YL) ACETONITRILE DERIVATIVES

PROCESS FOR THE PREPARATION OF a-(OXIMINO)- a-(1-AZABICYCLO 2.2.2 OCT- 3-YL) ACETONITRILE DERIVATIVES

机译:制备α-(肟基)-α-(1-氮杂双环[2.2.2] OCT-3-YL)乙腈衍生物的方法

摘要

A process for the preparation of a compound of the formula or a pharmaceutically acceptable salt thereof wherein R1 represents in which r represents 2, s represents 2 and t represents 0; R2 is group OR4, where R4 is hydrogen, C1-4 alkyl, C2-4 alkenyl or C2-4 alkynyl or R2 is a group OC(O)R5 where R5 is hydrogen or R4; and R3 is CN; said process comprising reacting a compound of the formula wherein R1( is R1 or a group convertible thereto, and R3( is CN, with a source of nitrous acid, and thereafter optionally or as necessary converting the resulting -NOH group to other -NR2 wherein R2 is as defined in formula (I), converting R1( when other than R1 to R1 and thereafter optionally forming a salt, provided that when R2 is other than OH, the salt is a pharmaceutically acceptable salt. Claimed as new is the crystalline 258 י" ג בתמוז התש" ס - July 16, 2000
机译:式I化合物或其药学上可接受的盐的制备方法,其中R 1代表其中r代表2,s代表2,t代表0。 R2为基团OR4,其中R4为氢,C1-4烷基,C2-4烯基或C2-4炔基,或R2为基团OC(O)R5,其中R5为氢或R4; R3为CN;所述方法包括使下式的化合物与亚硝酸源反应,其中R 1(为R 1或可转化为其的基团,且R 3(CN)为式的化合物与亚硝酸源,然后任选地或根据需要将所得的-NOH基团转化为其他-NR 2, R2如式(I)中所定义,将R1(当不是R1时转化为R1,然后任选地形成盐,条件是当R2不是OH时,该盐是药学上可接受的盐。声称是新的结晶258 י“גבתמוזהתש”ס-2000年7月16日

著录项

  • 公开/公告号IL114522B

    专利类型

  • 公开/公告日2000-07-16

    原文格式PDF

  • 申请/专利权人 SMITHKLINE BEECHAM PLC;

    申请/专利号IL114522

  • 发明设计人

    申请日1995-07-10

  • 分类号C07D453/02;

  • 国家 IL

  • 入库时间 2022-08-22 01:56:08

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