The invention relates to a process and intermediates for the preparation of enantiomerically pure cycloalkanoindolecarboxylic acids and azaindolecarboxylic acids and pyrimido\x9b1,2a!indolecarboxylic acids and their activated derivatives, characterized in that the tolyl acetic acid is first esterified with a chiral alcohol, then diastereoselective substitution at .alpha.-carbon atoms is carried out and this product is halogenated in the tolyl group and then reacted with appropriate cycloalkanoindoles, cycloalkanoazaindoles or pyrimido\x9b1,2a!indoles. It is possible by this method to prepare specifically, in high purity, the enantiomerically pure carboxylic acids which are intermediates for valuable medicaments.
该发明涉及一种制备对映纯环烷基
吲哚羧酸和氮杂
吲哚羧酸以及
嘧啶类
吲哚羧酸及其活性衍
生物的过程和中间体,其特点在于对甲
苯乙酸首先与手性醇酯化,然后在α-碳原子处进行立体选择性取代,将产物在
对甲苯基上卤代,然后与适当的环烷基
吲哚、环烷基氮杂
吲哚或
嘧啶类
吲哚反应。通过这种方法可以专门、高纯度地制备对映纯
羧酸,这些
羧酸是有价值的药物的中间体。