非金属路易斯酸催化的双吲哚甲烷类生物碱合成工艺研究

Synthesis of Bis(indolyl) Alkane Alkaloids Catalyzed by Non-Metallic Lewis Acid

以吲哚(1)和芳香醛(2)类为原料,B(C_(6)F_(5))_(3)为催化剂,在二氯甲烷(DCM)中制备双吲哚甲烷类生物碱,对反应温度、溶剂、n(1)∶n(2)比等工艺参数进行优化,并进行了克级放大。结果表明,在最优条件下[DCM作溶剂, 40℃,4 h,n(1)∶n(2)=1.1∶0.5,x((B(C_(6)F_(5))_(3))=1%],双吲哚甲烷类生物碱3a~3d产率为79%~93%。

Using indole(1) and aromatic aldehydes(2) as raw materials and B(C_(6)F_(5))_(3) as catalyst, bis(indolyl) alkane alkaloids were prepared in dichloromethane(DCM). The process parameters such as reaction temperature, solvent and n(1)∶n(2) were optimized, and the gram-scale amplification was carried out.The results showed that under the optimum conditions [DCM,40 ℃,4 h, n(1)∶n(2)=1.1∶0.5,x(B(C_(6)F_(5))_(3))=1%], the yields of bis(indolyl) alkane alkaloids 3 a~3 d was 79% to 93%.