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Process for the preparation of 1H-pyrrole-2-acetic esters

机译:1H-吡咯-2-乙酸酯的制备方法

摘要

A process for the preparation of esters of 1H-pyrrol-2-acetic acids of the formula IMAGE I wherein R1 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms and R2 is selected from the group consisting of alkyl of 1 to 4 carbon atoms and aralkyl of 1 to 4 alkyl carbon atoms comprising reacting a compound of the formula IMAGE II wherein R3 is selected from the group consisting of -CN and IMAGE in an aqueous media with a saponification base wherein the saponification base is added gradually to the 1H-pyrrol-2-acetonitrile and/or 1H-pyrrol-2-acetamide to selectively saponify the same to obtain a substantially isomer-free salt of 1H-pyrrol-2-acetic acid, adding alkali metal bicarbonate to the solution to keep the pH of solution at about 10.2 to 10.5 and reacting the salt of 1H-pyrrol-2-acetic acid without isolation and without removal of any water with a solution of an alkylating or aralkylating agent in an organic water-insoluble solvent in the presence of a phase transfer agent to obtain the ester of formula I in excellent yields and purity.
机译:制备式 I的1H-吡咯-2-乙酸的酯的方法,其中R1选自氢和1-4个碳原子的烷基,R2选自含1-4个碳原子的烷基和1-4个烷基碳原子的芳烷基,包括式 II的化合物,其中R3选自-CN和,其在水性介质中具有皂化碱其中将皂化碱逐渐加入到1H-吡咯-2-乙腈和/或1H-吡咯-2-乙酰胺中以对其进行选择性皂化以获得基本上无异构体的1H-吡咯-2-乙酸盐,将碱金属碳酸氢盐加入溶液中,以使溶液的pH值保持在约10.2至10.5,并使1H-吡咯-2-乙酸的盐发生反应,而无需分离,也不会在烷基化或芳烷基化剂的有机溶液中去除任何水水不溶性溶剂在相转移剂的存在下以优异的产率和纯度获得式I的酯。

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