您的位置: 首页 > 农业专利 > 详情页

专利权人:
LES LABORATOIRES SERVIER
发明人:
JEAN-MICHEL LERESTIF,JEAN-PIERRE LECOUVE,NICOLAS ROBERT,MARINA GAILLARD,LOIC MEUNIER (FINADO),PHILIPPE LETELLIER,MATHIEU BOIRET
申请号:
MX2012006525
公开号:
MX2012006525A
申请日:
2012.06.07
申请国别(地区):
MX
年份:
2013
代理人:
摘要:
Synthesizing 4-{3-[cis-hexahydrocyclopenta[c]pyrrol-2(1H)-yl]propoxy} benzamide hydrochloride (I), comprises reacting 2-methoxy-1-[2-(2-methoxy-acetyl)-cyclopentyl]-ethanone (II) with an ammonia to form tetrahydro-cyclopenta[c]pyrrole-1,3-dione (III), reducing (III) to yield octahydro-cyclopenta[c]pyrrole (IV), which is subsequently subjected to: either a coupling reaction with a benzamide compound (V) or a reductive amination with a benzamide compound (VI) to give free base of (I), which is soaked in hydrochloric acid to form (I) i.e isolated in the form of a solid. Synthesizing 4-{3-[cis-hexahydrocyclopenta[c]pyrrol-2(1H)-yl]propoxy} benzamide 4-{3-[cis-hexahydrocyclopenta[c]pyrrol-2(1H)-yl]propoxy}ben zamide hydrochloride (I), comprises reacting 2-methoxy-1-[2-(2-methoxy-acetyl)-cyclopentyl]-ethanone (II) with an ammonia, where the reaction mixture is then subjected to pyrolysis, at a temperature of greater than 100[deg] C to form tetrahydro-cyclopenta[c]pyrrole-1,3-dione (III), reducing (III) to yield (3aR,6aS)-octahydro-cyclopenta[c]pyrrole (IV), which latter compound is subsequently subjected: either to a coupling reaction, under basic conditions in a polar medium, with a benzamide compound of formula (V) or to a reductive amination with a benzamide compound of formula (VI) to give free base of (I), which is soaked in hydrochloric acid to form (I) i.e. isolated in the form of a solid. Y1 : -CH 2-Hal or -CH 2-OSO 2-R Hal : halo R : 1-6C alkyl or -C 6H 4-CH 3 either R1a, R2a : 1-6C alkyl or R1aR2a : -(CH 2) n- and n : 2-3, where one of R1a and R2a is H and the other is 1-6C alkyl. Independent claims are included for: (1) a crystalline form-I of (I) having an X-ray diffraction pattern on powder having diffraction lines as given in the specification and (2) a composition comprising (I) in combination with one or more inert vehicles. [Image] - ACTIVITY : Nootropic Dermatological Neuroprotective Antiparkinsonian Cerebroprotective Antialcoholic Vasotropic Tranquilize
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

意 见 箱

匿名:登录

个人用户登录

找回密码

第三方账号登录

忘记密码

个人用户注册

必须为有效邮箱
6~16位数字与字母组合
6~16位数字与字母组合
请输入正确的手机号码

信息补充