Intermediates for the synthesis of benzimidazole derivatives and a process for the preparation thereof

   
   

This invention provides a process for the preparation of a benzimidazole derivative (I) or a pharmaceutically acceptable salt thereof, ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxyl, etc., R.sup.2 is C.sub.1 -C.sub.6 alkyl, and R.sup.3 is hydrogen or a protecting group, which exhibits excellent hyopoglycemic action, said process comprising condensation of an amine derivative (III) with a carboxylic acid derivatives (II) to afford a compound (IV), followed by cyclization of compound (IV) in the presence of an acid.

Esta invenção fornece um processo para a preparação de um derivative do benzimidazole (I) ou um sal pharmaceutically aceitável disso, ## do ## STR1 wherein R.sup.1 é C.sub.1 - C.sub.6 alkyl, C.sub.1 - C.sub.6 alkoxyl, etc., R.sup.2 é C.sub.1 - o alkyl C.sub.6, e R.sup.3 são hidrogênio ou um grupo protegendo, que exiba a ação hyopoglycemic excelente, processo dito que compreende a condensação de um derivative do amine (iii) com os derivatives ácidos carboxylic (ii) para ter recursos para um (iv) composto, seguida pelo cyclization do composto (iv) na presença de um ácido.

 
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