Department of Chemistry, National University of Singapore , 3 Science Drive 3, Singapore 117543.
J Org Chem. 2014 May 16;79(10):4644-9. doi: 10.1021/jo500609a. Epub 2014 Apr 25.
N-Bromosuccinimide-induced electrophilic multicomponent reaction has been applied to the synthesis of Reboxetine intermediate, a highly potent selective norepinephrine reuptake inhibitor. By simply changing the olefinic partner, the synthesis of a carnitine acetyltransferase inhibitor, which contains a 2,6,6-trisubstituted morpholine system, can be accomplished.
N-溴代丁二酰亚胺诱导的亲电多组分反应已被应用于瑞波西汀中间体的合成,瑞波西汀是一种高效选择性去甲肾上腺素再摄取抑制剂。通过简单地改变烯烃配体,即可完成肉碱乙酰转移酶抑制剂的合成,其中包含 2,6,6-三取代吗啉系统。