Department of Chemical Development, Boehringer Ingelheim Pharmaceuticals Inc., Ridgefield, Connecticut 06877, USA.
Org Lett. 2010 Mar 5;12(5):1104-7. doi: 10.1021/ol1000999.
A series of structurally novel, operationally convenient, and efficient chiral 2-phosphino-2,3-dihydrobenzo[d][1,3]oxaphosphole ligands was developed. Applications of ligands 3a and 3b in rhodium-catalyzed asymmetric hydrogenation of alpha-(acylamino)acrylates and beta-(acylamino)acrylates provided excellent enantioselectivities (up to >99% ee) and reactivities (up to 10,000 TON).
开发了一系列结构新颖、操作方便、高效的手性 2-膦基-2,3-二氢苯并[d][1,3]氧杂磷杂环戊烯配体。配体 3a 和 3b 在铑催化的α-（酰氨基）丙烯酰胺和β-（酰氨基）丙烯酰胺的不对称氢化反应中的应用，提供了极好的对映选择性（高达>99%ee）和反应活性（高达 10000TON）。
