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

摘要

A method for preparing an N-hydroxysuccinimide ester derivative is provided to obtain the N-hydroxysuccinimide ester derivative within short period of time with high yield and high purity under mild condition without producing any side products and 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. In the formulae, R is substituted or unsubstituted alkyl or substituted or unsubstituted aryl. In the method, the amount of the diphosgene used is 0.5-1.0 mol times regarding the carboxylic acid.