用户名: 密   码:
注册 | 忘记密码?
专利详细信息
专利号
HU229396B1
专利标题 New process for the preparation of (2s,3as,7as)-1-[(s)-alanile]octahydro-1h-indole-2-carboxy acid derivatives and their use for synthesing perindopril
专利权人 LES LABORATOIRES SERVIER;
发明人 Mezei, Tibor;Porcs-makkay, Marta;Simig, Gyula;
申请号 HU20020002437
申请日 2002/7/24
公开日 2013/11/28
优先权号
IPC C07B06100000;
专利类型
法律状态查询 查看法律状态


Process for industrial synthesis of (2S 3aS 7aS)-1-(S) alanyl octahydro-2-carboxylic acid derivatives (I) by reaction of alanine derivative (VI) and ester derivative (V) and catalytic hydrogenation. Process for industrial synthesis of (2S 3aS 7aS)-1-(S) alanyl octahydro-2-carboxylic acid derivatives of formula (I) comprises reaction of an ester of formula (V) with an alanine of formula (VI) in an organic solvent optionally in the presence of less than 0.6 mole per mole (V) of 1-hydroxybenzotriazole and in the presence of 1-1.2 mole of dicyclohexylcarbodiimide and 1-1.2 mole of triethylamine per mole of (V) at 20-50 degrees C to give a compound of formula (VII) which is then hydrogenated at 1-40 bars and 30-70 degrees C in the presence of a catalyst preferably rhodium on charcoal or platinum dioxide to form (I). R1 = H 1-6C alkyl or benzyl; and R2 = amino protecting group. An Independent claim is also included for a process for the synthesis of perindopril starting from (I).
没有相关的数据
没有相关的数据
引证图片
暂无附图

注:除CN专利外,本系统默认提供的所有其他中文标题和摘要来自机器翻译。

上传 | 编辑 | 标注(0) | 下载专利全文 | 收藏