抗肿瘤化合物6-溴代吲哚-3-甲醇的设计合成

Design Synthesis and Application of Anti-tumor Compound 6-Bromo-Indole-3-Carbinol

以邻硝基甲苯为原料,通过溴化、类羟醛缩合、成环、甲酰化和还原等步骤合成6-溴代吲哚-3-甲醇,总收率26.5%,所有化合物的结构均经核磁共振谱(NMR)、质谱(ESI-MS)等方法确证。以标题化合物为结构框架,合成系列6-位取代的吲哚-3-甲醇衍生物,可获得类药性好的化合物。

Applying o-nitrotoluent as starting material, 6-bromo-indole-3-carbinol was synthesized via multiple-step reactions including bromidation, aldol-like condensation, cyclization, Vilsmeier-Haack formylation and reduction. The overall yield reaches 26.5%. The structures of all the products have been confirmed by ESI-MS and NMR. Based on the scaffold of the title compound, series of 6-substituted in- dole-3-carbinols can be prepared in search for the better drug-like compounds.