School of Chemistry, The University of Manchester, Oxford Road, Manchester, M13 9PL, UK.
Department of Oncology, AstraZeneca, Darwin Building, Cambridge Science Park, Milton Road, Cambridge, CB4 0WG, UK.
Angew Chem Int Ed Engl. 2017 Apr 3;56(15):4183-4186. doi: 10.1002/anie.201612445. Epub 2017 Mar 13.
A metal-free aminoarylation of internal alkynes is described, yielding tetrasubstituted enaminoates. The transformation proceeds in good to excellent yields through a tandem conjugate addition/Smiles rearrangement involving aryl and heteroaryl sulfonamides. Substrate scope is very broad under simple, user-friendly conditions, and the reaction can be used to easily access biologically active phenethylamine derivatives.
本文描述了一种无金属的芳基炔烃的氨基芳基化反应，生成了四取代的烯胺酸酯。该转化通过串联的共轭加成/Smiles 重排反应，涉及芳基和杂芳基磺酰胺，以良好至优秀的收率进行。在简单、用户友好的条件下，底物的适用范围非常广泛，并且该反应可用于轻松获得生物活性的苯乙胺衍生物。
