α-烷基苯乙酰胺的合成新方法

A Novel Method for The Synthesis ofα-Alkylated Arylacetamides

以各种取代的N-Boc氧化吲哚(1)为起始原料,在氨水中室温条件下发生开环反应,获得合成了14个新颖的α-烷基苯乙酰胺2a~2n,产率67%~91%,其结构经^(1)H NMR,^(13)C NMR和HR-MS(ESI-TOF)表征,并且经过单晶2e进一步确定了其结构。产物可作为后续天然产物或药物分子合成的中间体,也可为生物活性筛选提供物质基础。

Fourteenα-alkylated arylacetamides(2a~2n)were synthesized via a ring-opening reaction of N-Boc oxindoles(1)with ammonia under room temperature conditions for 10 h.The yields were 67%~91%.The structures of products were characterized by ^(1)H NMR,^(13)C NMR and HR-MS(ESI-TOF),and further confirmed by X-ray crystallographic study of single crystal of 2e.The synthesized products can be used as intermediates for subsequent natural products or drug molecular synthesis,and also provide material basis for biological activity screening.