NOVEL PROCESS FOR THE PREPARATION OF N-HYDROXYSUCCINIMIDE ESTER DERIVATIVES

摘要

A novel process for the preparation of N-hydroxysuccinimide ester derivatives is provided to prepare the compounds under mild conditions, reduce the reaction steps and process time, and easily separate and purify the target compounds without environmental pollution caused by by-products. The N-hydroxysuccinimide ester derivatives represented by the formula(I) are prepared by reacting carboxylic acid represented by the formula(II) with N-hydroxysuccinimide in the presence of triphosgene, wherein R is optionally substituted alkyl or optionally substituted aryl group. The N-hydroxyphthalimide ester represented by the formula(IV) is prepared by reacting carboxylic acid represented by the formula(II) with N-hydroxyphthalimide represented by the formula(III) in the presence of triphosgene.