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METHOD OF ENANTIOSELECTIVE SYNTHESIS OF INTERMEDIATE COMPOUNDS USED IN SYNTHESIS OF FLAVONE-SUBSTITUTED PYRROLIDINES

机译:对映体合成用于黄酮取代的吡咯烷酮的中间化合物的合成方法

摘要

FIELD: chemistry.;SUBSTANCE: invention relates to enantioselective synthesis of intermediate compounds, specifically (-)-trans-(1-methyl-3-(2,4,6-trimethoxyphenyl) pyrrolidin-2-yl)methanol of formula A ; involving steps on which (-)-trans-1-methyl-5-oxo-3-(2,4,6-trimethoxyphenyl)pyrrolidin-2-carboxylic acid of formula E is treated with a reducing agent in a solvent. These compounds are used in synthesis of the (+)-trans enantiomer of pyrrolidines substituted with flavones, having formula 1 , or salts thereof which are cycline-dependant kinase inhibitors and can be used to treat proliferative disorders such as cancer.;EFFECT: method allows efficient large-scale synthesis of the compound by excluding the racemate splitting technique.;15 cl, 12 ex
机译:中间体化合物的对映选择性合成技术领域本发明涉及中间体化合物的对映选择性合成,特别是式A的(-)-反式-(1-甲基-3-(2,4,6-三甲氧基苯基)吡咯烷-2-基)甲醇图片文件=“ 00000014.GIF” he =“ 57” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 40” />;涉及步骤,其中式E的(-)-trans-1-methyl-5-oxo-3-(2,4,6-三甲氧基苯基)吡咯烷-2-羧酸<图像文件=“ 00000015.GIF” he =“在溶剂中用还原剂处理57“ imgContent =” undefined“ imgFormat =” GIF“ wi =” 41“ />。这些化合物用于合成被黄酮取代的吡咯烷的(+)-反式对映异构体,具有式1 或其盐,它们是细胞周期蛋白依赖性激酶抑制剂,可用于治疗增生性疾病,例如癌症。;效果:该方法可通过排除外消旋体拆分技术有效地大规模合成化合物; 15 cl ,12前

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