[EN] PROCESS FOR PREPARING NATEGLINIDE AND INTERMEDIATES THEREOF<br/>[FR] PROCEDE DE PREPARATION DE NATEGLINIDE ET DE SES INTERMEDIAIRES
申请人:TEVA PHARMA
公开号:WO2004005240A1
公开(公告)日:2004-01-15
Provided is a process for preparation of an intermediate in the synthesis of nateglinide. Trans-4-isopropylcyclohexane acid chloride is formed by reacting 4-isopropylcyclohexanecarboxyl acid with thionyl chloride in the presence of an effective amount of an organic amide. Also provided are processes for preparation of nateglinide by acylation of a suitable salt of D-phenylalanine with trans-4-isopropylcyclohexane acid chloride in both a single and a two phase system, and in water free of a co-solvent.
提供了一种合成那格列奈中间体的制备过程。通过在有机酰胺的有效量存在下,将4-异丙基环己基甲酸与氯化亚砜反应,形成反式-4-异丙基环己烷甲酸氯化物。还提供了一种通过在单相和两相系统中,以及在不含共溶剂的无水条件下,将D-苯丙氨酸的适当盐与反式-4-异丙基环己基甲酸氯化物酰化的那格列奈制备过程。