Johnson Chad R, Ansari Mohd Imran, Coop Andrew
Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 N. Pine Street, Baltimore, Maryland 21201, United States.
ACS Omega. 2018 Sep 30;3(9):10886-10890. doi: 10.1021/acsomega.8b01426. Epub 2018 Sep 10.
A rapid, transition metal-free, high-yielding, tetrabutylammonium bromide-promoted method of N-arylation is reported within. The optimized conditions tolerated a wide range of secondary amines and was equally effective with bromo- and chlorobenzene-including substituted aryl halides. The developed method is found to be effective for N-arylation when compared to earlier methods which involve harsh conditions, transition metals, lack of scalability, and long reaction times. Our method utilizes conventional heating only; it is readily scalable; and the products are facile to purify.
本文报道了一种快速、无过渡金属、高产率、由溴化四丁基铵促进的N-芳基化方法。优化后的条件能耐受多种仲胺，对溴苯和氯苯（包括取代芳基卤化物）同样有效。与早期涉及苛刻条件、过渡金属、缺乏可扩展性和长反应时间的方法相比，所开发的方法被发现对N-芳基化有效。我们的方法仅使用常规加热；易于扩展；并且产物易于纯化。
