1位置換ピロール−3−カルボン酸誘導体の製造法

Production of 1-position substituted pyrrole-3-carboxylic acid derivative

Abstract

(57)【要約】 【課題】 簡便でかつ工業的にも十分に満足いく収率で 1位置換ピロール−3−カルボン酸誘導体を製造する方 法を提供する。 【解決手段】 次の式、 【化1】 (式中、R 1 およびR 2 は同一または異なってアルキル、 アラルキルまたはアリール基を示す)に従い、式(II) で表される化合物に、式(III)で表される化合物と酸 無水物を作用させることを特徴とする式(I)で表され る1位置換ピロール−3−カルボン酸誘導体の製造法。
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.

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