Process for the preparation of carboxylic acid succinimidyl esters

摘要

(1) Production of carboxylic acid succinimidyl esters (II) comprises (a) reaction of N-hydroxysuccinimide (III) with a carboxylic acid (IV) and a halophosphoric acid ester of formula (R1O)(R2O)P(O)Cl (I) in the presence of a base and solvent at 0-100 degrees C; and (b) isolating (II). R1, R2 = 2-6C alkyl or Ph; or R1+R2 form a 6C aryl residue. Also claimed is (2) the production of products of (II) by carrying out step (a) as above, and reacting the reaction mixture obtained with a nucleophile (V) suitable for acylation.