摘要
这份报纸描述一条简明、实际的线路到 enantiomerically 充实的 5 烷基代替的烟碱类似物。Vilsmeier 反应被用来构造器官的硼试剂和 pyrrolidine 戒指的环合 chiral homoallylic 白酒的介绍通过 chiral 叠氮化物的减小跟随的 nicotinaldehydes 戒指。17 类似物被综合了,他们的相应生物活动被测试,在哪个混合物 10d 和 10g 对 RD 和 SY-SY5Y 展出优秀 IC50 价值。
This paper describes a concise and practical route to enantiomerically enriched 5-alkyl substituted nicotine analogs. The Vilsmeier reaction was used to construct the nicotinaldehydes ring followed by the introduction of the chiral homoallylic alcohol by organic boron reagent and the cyclization of the pyrrolidine ring through the reduction of a chiral azide. 17 analogs have been synthesized and their corresponding biological activities were tested, in which compounds 10d and 10g exhibit excellent ICs0 values against RD and SY-SY5Y.