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新型避孕药RU 486(本刊1986,17:395)的合成过程中,是用4-溴-N,N-二甲基苯胺(1)在11-位引入对-(N,N-二甲胺基)苯基的1的合成方法似以N,N-二甲基苯胺的对位直接引入溴较为简洁,但是芳胺和酚类用溴素进行溴化,存在易发生多溴代产物、邻对位溴代选择性不强以及底物易被氧化等缺点。据Calo等报道,2,4,4,6-四溴环己-2,5-二烯酮(2)是一种具区域选择性的对位单溴化试剂[J Chem Soc (C)1971,21:3653]该试剂制备方便,与伯-、仲-或叔-苯胺化合物反
The new contraceptive RU 486 (1986, 17: 395) was synthesized by the introduction of p- (N, N-dimethyl Amino) phenyl 1 like the synthesis of N, N-dimethylaniline direct introduction of bromine is more concise, but aromatic amines and phenols brominated with bromine, prone to polybrominated products, Adjacent bromine selectivity is not strong and the substrate is easily oxidized and other shortcomings. According to Calo et al., 2,4,4,6-tetrabromocyclohexa-2,5-dienone (2) is a regioselective regiobrominated reagent [J Chem Soc (C) 1971 , 21: 3653] This reagent is conveniently prepared to react with primary-, secondary- or tertiary-aniline compounds