Novel process for preparation of 5-hydroxy-5-aryl-pyrrole-2-ones and intermediates thereof

The present invention relates to a process for the preparation of 5-hydroxy-5-aryl-pyrrol-2-ones of formula (I) from an arylated furanone intermediate of formula (II). The present invention relates to a two-stage process for the preparation of 5-hydroxy-5-aryl-pyrrole-2-ones, in particular, 4-chloro-5-hydroxyl-1-substituted-5-arylated-1H-pyrrole-2 (5H)-ones, and to a method for the preparation of 5-hydroxyl-5-aryl-pyrrole-2-ones. In a first stage, an arylated furanone intermediate of formula (II) is prepared by a Lewis acid catalyzed Friedel Crafts reaction in the presence of a haloalkane solvent. In the second stage, the final compound of formula (I) is obtained by a lactonization reaction from the arylated furanone intermediate in the presence of a combination of a primary amine and a tertiary amine. # imgabs0 # 本发明涉及一种用于由式(II)的中间体芳基化的呋喃酮制备式(I)的5-羟基-5-芳基-吡咯-2-酮的工艺。本发明涉及用于制备5-羟基-5-芳基-吡咯-2-酮，特别是4-氯-5-羟基-l-取代的-5-芳基化的-1H-吡咯-2(5H)-酮的两阶段工艺。在第一阶段中，式(II)的芳基化的呋喃酮中间体在存在卤代烷烃溶剂的情况下通过路易斯酸催化的Friedel Crafts反应制备。在第二阶段中，在存在