NEW SYNTHETIC METHOD OF GLYCOPYRROLATE AND PHARMACEUTICAL FORMULATIONS CONTAINING THIS ACTIVE INGREDIENT

摘要

The present invention relates to a method for synthesizing RS and Sr racemic glycopyrrolate represented by structural formula I by makingα-cyclopentylmandelic acid racemic body (R/S racemic) represented by structural formula 3 react with 1-methyl-3-pyrrolidinol methyl bromide represented by structural formula 5. In the novel method for synthesizing glycopyrrolate of the present invention, by-products produced during reaction can be easily removed through crystallization, purification process can be facilitated, synthesizing time can be reduced, and glycopyrrolate optimized for 35 regulations in US pharmacopoeial forum can be synthesized. In addition, collection of unreacted substance can be facilitated, yield of RS or SR glycopyrrolate can be increased by reusing RR or SS glycopyrrolate so that the yield can be more increased by the collection method. [Reference numerals] (AA) Standard Glycopyrrolate