首页> 外国专利> Method for preparing acid (+) - 1,4 - dihydro - 7 - (3S, 4S) - 3 - methoxy - 4 - (methylamino) - 1 - pirrolidinil - 4 - oxo - 1 - (2 - thiazolyl) - 1.8 - naftiridin - 3 - carboxylic acid

Method for preparing acid (+) - 1,4 - dihydro - 7 - (3S, 4S) - 3 - methoxy - 4 - (methylamino) - 1 - pirrolidinil - 4 - oxo - 1 - (2 - thiazolyl) - 1.8 - naftiridin - 3 - carboxylic acid

机译:制备酸(+)-1,4-二氢-7-[(3S,4S)-3-甲氧基-4-(甲氨基)-1-吡咯烷]-4-羰基-1-(2-噻唑基)-的方法1.8-萘菲丁-3-羧酸

摘要

2. Prepare acid (+ - 1,4-dihydro-7 - [(3S, 4S) - 3-methoxy-4 - (methylamine) - 1-pyridine-1 - (2-thiazolpidan) - 1,8-naftiridin-3-carboxyl; A pharmaceutical component containing (+ - 1,4-dihydro-7 - [(3S, 4S) - 3-methoxy-4 - (methylamine) - 1-pirolidine is also provided.(l) 4-oxo-1 - (2-tiazolyl) - 1,8-nafeldin-3-carboxyl and the treatment method using these compounds. 1. Characteristic 1: a product for the production of (+ - 1,4-dihydro-7 - [(3S, 4S) - 3-methoxy-4 - (methylamine) - 1-pyridyl-4 -- 4 - (methylamine) - 1-hydroxy-1 - (2-thiazolidine) - 1,8-nafiridin-3-carboxycharacterized in that it comprises: i) opening the epoxide of compound 3 with methylamine to obtain compound 4, ii) resolving compound 4 with a chiral acid selected from L - (-) malic acid and L - (-) - pyroglutamic acid to obtain compound 5A or 5B, iii) protecting the secondary amine of compound 5A or 5B with the tert-butoxycarbonyl protecting group to obtain compound 6, iv) methylating the free hydroxyl group of compound 6 with a methylating agent,v) desproteger los grupos amino con monohidrato de cido p-toluensulf nico para obtener el compuesto 8 y vi) hacer reaccionar el compuesto 8 con el Compuesto 10 para obtener cido (2B) -1 4-dihidro-7- (3S 4S) - iii) protect the secondary amine of compound 5A or 5B with the tert-butoxycarbonyl protecting group to obtain compound 6, iv) methylate the free hydroxyl group of compound 6 with a methylating agent, and v) deprotect the amino groups with acid monohydrate p-toluenesulfonic to obtain compound 8.
机译:2.制备酸(+-1,4-二氢-7-[(3S,4S)-3-甲氧基-4-(甲胺)-1-吡啶-1-(2-噻唑烷)-1,8-萘替丁- 3-羧基;还提供了含有(+ 1,4-二氢-7-[(3S,4S)-3-甲氧基-4-(甲胺)-1-吡咯烷)的药物成分。(l)4-氧代- 1-(2-噻唑基)-1,8-萘菲丁-3-羧基和使用这些化合物的处理方法1.特征1:一种用于生产(+-1,4-二氢-7-[(3S)的产品,4S)-3-甲氧基-4-(甲胺)-1-吡啶基-4-4-(甲胺)-1-羟基-1-(2-噻唑烷)-1,8-萘啶-3-羧基其包括:i)用甲胺打开化合物3的环氧化物以获得化合物4,ii)用选自L-(-)苹果酸和L-(-)-焦谷氨酸的手性酸拆分化合物4以获得化合物5A或5B,iii)用叔丁氧羰基保护基保护化合物5A或5B的仲胺以获得化合物6,iv)甲基化com的游离羟基磅6与甲基化剂一起使用,v)腐烂剂los grupos氨基吡啶单聚对甲基苯磺酸对氨基苯甲酸乙酯8 y vi)对乙酰氨基苯甲酸乙酯8 con el Compuesto 10对羟基苯甲酸乙酯(2B)-1 4-二甲基- 7-(3S 4S)-iii)用叔丁氧羰基保护基保护化合物5A或5B的仲胺以获得化合物6,iv)用甲基化剂甲基化化合物6的游离羟基,和v)脱保护将氨基与酸一水合物对甲苯磺酸制得化合物8。

著录项

  • 公开/公告号AR074962A1

    专利类型

  • 公开/公告日2011-02-23

    原文格式PDF

  • 申请/专利权人 SUNESIS PHARMACEUTICALS INC.;

    申请/专利号AR2009P105186

  • 发明设计人

    申请日2009-12-30

  • 分类号C07D471/04;A61K31/4375;A61P35;

  • 国家 AR

  • 入库时间 2022-08-21 18:07:27

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号