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

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 mild condition within one hour without requiring preparation of a coupling reagent for introducing a hydroxysuccinimide group. To prepare an N-hydroxysuccinimide ester derivative represented by the formula(I), a carboxylic acid represented by the formula(II) is reacted with N-hydroxysuccinimide in the presence of diphosgene and triphenylphosphine, wherein the amount of the diphosgene used is 0.5-1.0 mol times regarding the carboxylic acid. In the formula(I) and (II), R is substituted or unsubstituted alkyl or substituted or unsubstituted aryl.