PRODUCTION OF 1-POSITION SUBSTITUTED PYRROLE-3-CARBOXYLIC ACID DERIVATIVE

PROBLEM TO BE SOLVED: To obtain a pyrrole-3-carboxylic acid derivative useful as a medicine, its synthetic raw material and its intermediate simply in a short time in high yield by using an N-substituted formyl-glycine as a raw material. SOLUTION: A compound of formula I (R1 is an alkyl, an aralkyl or an aryl) is reacted with a compound of the formula, HC≡C-COOR2 (R2 is an alkyl, an aralkyl or an aryl) and an acid anhydride (e.g. acetic anhydride) at 80 deg.C to a reflux temperature for 4-24 hours with stirring to give a 1-position substituted pyrrole-3-carboxylic acid derivative of formula II. The compound of formula I in an amount of 1mol is reacted with >=1mol of the acid anhydride and 1-5mols of the compound of the formula, HC≡C-COOR2 . Since the reaction is not a substitution reaction on the pyrrole ring, production of pyrrole-2- carboxylic acid derivative as a by-production will not occur and a complicated separating process is not required. Since a dangerous reagent is not used, procedures are simple and reaction processed are a few and a time required for the synthesis can be shortened.