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).
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