State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University , Haihe Education Park, 38 Tongyan Road, Tianjin 300353, People's Republic of China.
Org Lett. 2017 Dec 1;19(23):6344-6347. doi: 10.1021/acs.orglett.7b03186. Epub 2017 Nov 17.
Bromide-mediated intermolecular annulation of phenylethanone derivatives with alkynes has been developed, which allows for the regioselective formation of polysubstituted 1-naphthols. The usage of readily available bromine catalyst, broad substrate scope, and mild conditions make this protocol very practical. Mechanistic investigations reveal that the bromination of phenylethanone derivatives occurs to yield bromo-substituted intermediates, which react in situ with alkynes to furnish the desired 1-naphthols.
溴化物介导的苯乙酮衍生物与炔烃的分子内环化反应已经被开发出来，该反应能够区域选择性地形成多取代的 1-萘酚。由于使用了易得的溴催化剂、广泛的底物范围和温和的反应条件，该方法具有很高的实用性。机理研究表明，苯乙酮衍生物的溴化反应生成了溴代中间体，这些中间体与炔烃原位反应生成所需的 1-萘酚。
