Piramal Discovery Solutions , Pharmaceutical Special Economic Zone , Sarkhej Bavla Highway , Ahmedabad , Gujarat 382213 , India.
Org Lett. 2018 Sep 7;20(17):5423-5426. doi: 10.1021/acs.orglett.8b02331. Epub 2018 Aug 16.
A highly regioselective and diastereoselective addition of 2-azaallyl anions to N- tert-butanesulfinylimines is reported. This methodology affords the preparation of enantiomerically and diastereomerically pure vicinal diamines bearing two adjacent stereocenters. Reactions proceed efficiently (yield up to 94%), diastereoselectively ( dr values up to 98:2:0:0), and site-selectively to deliver products with differentiated amino groups.
报道了 2-氮烯丙基负离子与 N-叔丁基亚磺酰亚胺的高区域选择性和立体选择性加成。该方法可制备具有两个相邻手性中心的对映体和非对映体纯的偕二氨基化合物。反应高效进行（产率高达 94%），立体选择性好（ dr 值高达 98:2:0:0），并且位点选择性好，可得到具有不同氨基的产物。
