Lee Anna, Younai Ashkaan, Price Christopher K, Izquierdo Javier, Mishra Rama K, Scheidt Karl A
Department of Chemistry, Center for Molecular Innovation and Drug Discovery, Chemistry of Life Processes Institute, Northwestern University , Silverman Hall, Evanston, Illinois 60208, United States.
J Am Chem Soc. 2014 Jul 30;136(30):10589-92. doi: 10.1021/ja505880r. Epub 2014 Jul 15.
A convergent, catalytic asymmetric formal [4 + 2] annulation for the synthesis of dihydroquinolones has been developed. Carboxylic acids can be employed as precursors to NHC enolates through an in situ activation strategy. Simultaneous generation of a reactive aza-o-quinone methide under the basic conditions employed for NHC generation leads to a dual activation approach.
已开发出一种用于合成二氢喹诺酮的收敛性、催化不对称形式的[4 + 2]环化反应。羧酸可通过原位活化策略用作NHC烯醇盐的前体。在用于生成NHC的碱性条件下同时生成活性氮杂邻醌甲基化物,从而导致双重活化方法。