<i>C</i>-Alkylation of <i>N</i>-alkylamides with styrenes in air and scale-up using a microwave flow reactor
作者:Joshua P. Barham、Souma Tamaoki、Hiromichi Egami、Noriyuki Ohneda、Tadashi Okamoto、Hiromichi Odajima、Yoshitaka Hamashima
DOI:10.1039/c8ob02282h
日期:——
N-alkylamides with styrenes is reported, proceeding in ambient air/moisture to give arylbutanamides and pharmaceutically-relevant scaffolds in excellent mass balance. Various amide and styrene derivatives were tolerated, rapidly affording molecular complexity in a single step; thus highlighting the future utility of this transformation in the synthetic chemistry toolbox. Reaction scalability (up to
Ç的烷基化Ñ -alkylamides与苯乙烯报道,在环境空气中前进/水分,得到arylbutanamides和在良好的质量平衡的药学上相关的支架。可以耐受各种酰胺和苯乙烯衍生物,只需一步即可快速提供分子复杂性。因此,突出了这种转变在合成化学工具箱中的未来实用性。作为使用苯乙烯连续流动的C-烷基化反应的第一个实例,使用微波流反应器证明了反应可扩展性(高达65 gh -1产物)。