Selective Synthesis of 4-Alkylidene-β-lactams and <i>N</i>,<i>N</i>′-Diarylamidines from Azides and Aryloxyacetyl Chlorides via a Ketenimine-Participating One-Pot Cascade Process
作者:Yun-Yun Yang、Wang-Ge Shou、Deng Hong、Yan-Guang Wang
DOI:10.1021/jo702733h
日期:2008.5.1
A one-pot cascade approach to 4-alkylidene-β-lactams and N,N′-diarylamidines from aryl azides and aryloxyacetyl chlorides has been developed. The chemical outcome of the reaction can be controlled selectively by an appropriate choice of the stoichiometric ratio of different substrates and reagents. The products should find use in pharmaceutical discovery, especially in the development of new antimicrobial
已开发出一锅级联方法从芳基叠氮化物和芳氧基乙酰氯制备4-亚烷基-β-内酰胺和N,N'-二芳基ary。该反应的化学结果能够选择性地由不同的底物和试剂的化学计量比的适当选择被控制。该产品应可用于药物开发,尤其是在针对耐多药病原体的新型抗菌剂的开发中。