吲哚生物碱Indiacen A的全合成研究

Total Synthesis of Indole Alkaloid Indiacen A

目的:采用4-溴吲哚为起始原料,探索完成具有异戊二烯基长链的酰基吲哚化合物Indiacen A的简捷高效全合成。方法:通过钯催化的Heck-脱水反应高效引入异戊二烯基侧链,并对反应条件进行优化筛选。结果:利用最优条件以91%的高产率“一锅法”完成了天然产物Indiacen A的合成。结论:开发了一种无保护基及原子经济的合成策略,操作简单,总产率高。

Objective:The concise and efficient total synthesis of Indiacen A,an acyl indole compound with long isoprene chain,was studied by 4-bromoindole as the starting material.Methods:The isoprene side chain was efficiently introduced through the Heckdehydration reaction catalyzed by palladium,and the reaction conditions were optimized and screened.Results:The natural product Indiacen A was synthesized by"one-pot method"with a high yield of 91%under optimal conditions.Conclusion:A synthesis strategy of protecting-group-free and atom economy has been developed,which is simple to operate and has a high overall yield.