首页> 外国专利> AN IMPROVED PROCESS FOR PREPARING 2-OXINDOLES OF FORMULA I, A KEY RAW MATERIAL FOR MAKING PHARMACEUTICAL DRUGS AND INTERMEDIATES THEREOF

AN IMPROVED PROCESS FOR PREPARING 2-OXINDOLES OF FORMULA I, A KEY RAW MATERIAL FOR MAKING PHARMACEUTICAL DRUGS AND INTERMEDIATES THEREOF

机译:一种改进的制备式Ⅰ的2-氧吲哚的方法,该式为制造药物的主要原料并中间体

摘要

The present invention provides an improved processes having practical utility for preparing 2-oxindoles of formula I comprising preparation of 2-nitroarylmalonate diester of formula II as first intermediate and subsequent insitu reductive cyclisation using metal acid combination and its modified work-up to form compound of formula I free from metal generated impurity of formula M(OH)X wherein M is metal cation and X is anion. R is selected from hydrogen, linear, branched or cyclic alkyl, aryl, substituted aryl, heteroaryl, haloalkyl like CF3, alkoxy, haloalkoxy, thioalkyl and halogen preferably chloro Formula I wherein R' and R" are same or different and is selected from linear.branched and cyclic alkyl (C1C4groups)preferably methyl R is selected from hydrogen, linear, branched or cyclic alkyl, aryl, substituted aryl, heteroaryl, haloalkyl like CF3, alkoxy, haloalkoxy, thioalkyl and halogen preferably chloro Formula II.
机译:本发明提供了一种具有实际实用性的改进的方法,用于制备式I的2-氧吲哚,包括制备式II的2-硝基芳基丙二酸酯二酯作为第一中间体,随后使用金属酸组合及其改性后处理进行原位还原环化以形成式I的化合物。式I不含金属生成的式M(OH)X杂质,其中M为金属阳离子,X为阴离子。 R选自氢,直链,支链或环状烷基,芳基,取代的芳基,杂芳基,卤代烷基如CF 3 Sub,烷氧基,卤代烷氧基,硫代烷基和卤素,优选氯代式I,其中R'和R“为相同或不同,并且选自直链和支链和环状烷基(C 1 C 4 基团),优选甲基R选自氢,直链,支链或环状烷基,芳基,取代的芳基,杂芳基,卤代烷基(如CF 3 Sub),烷氧基,卤代烷氧基,硫代烷基和卤素,优选为氯式II。

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