NOVEL METHOD FOR PREPARATION OF 4-SUBSTITUTED -1H-PYRROLE-3-CARBOXYLIC ACID ESTER

摘要

PURPOSE: Provided is a novel method for preparation of 4-substituted -1H-pyrrole-3-carboxylic acid ester, which is an intermediates in the preparation of an inhibitor for farnesyl transferase used in anti-cancer drugs, from the corresponding aldehyde compound through Horner-emmons reaction in high yield and purity. CONSTITUTION: A novel preparation method of 4-substituted -1H-pyrrole-3-carboxylic acid ester represented by formula (1) is composed of the followings: (a) reacting aldehyde compound of general formula (2) with trialkyl phosphono acetate of the formula (3) in the presence of 1 to 1,5 molar equivalent of alkali metal alkoxide based on the compound of the formula (2) in inert solvent, to prepare α, β-unsaturated ester compound formula (4); and (b) reacting the compound of the formula (4) with adding 1-1.5 molar equivalent of same base based TosMIC and the compound of the formula (4).