NOVEL PROCESS FOR THE PREPARATION OF N-HYDROXYSUCCINIMIDE ESTER DERIVATIVES BY USING TRIPHENYLPHOSPHINE AND TRIPHOSGENE

摘要

A method for preparing an N-hydroxysuccinimide ester derivative is provided to be able to obtain the N-hydroxysuccinimide ester derivative with high yield and high purity under normal pressure at room temperature without generating side produces. An N-hydroxysuccinimide ester derivative represented by the formula(I) is prepared by reacting a carboxylic acid represented by the formula(II) with N-hydroxysuccinimide in the presence of triphosgene and triphenylphosphine, wherein the amount of the triphosgene used is 0.4-1.0 mol times regarding the carboxylic acid. In the formulae, R is substituted or unsubstituted alkyl or substituted or unsubstituted aryl.