Centre for Semiochemicals and ‡Laboratory of X-ray Crystallography, CSIR-Indian Institute of Chemical Technology , Hyderabad, 500 007, India.
Org Lett. 2017 Jan 6;19(1):170-173. doi: 10.1021/acs.orglett.6b03473. Epub 2016 Dec 23.
An efficient enantioselective α-amination of 2-substituted 3-indolinones has been achieved for the first time using hydroquinidine as a chiral catalyst through an aza-Michael reaction. The desired α-hydrazino esters are obtained in excellent yields with high enantiomeric excess leading to a quaternary stereocenter with a broad substrate scope.
首次使用氢奎宁作为手性催化剂，通过氮杂迈克尔加成反应，实现了 2-取代 3-吲哚啉酮的高效对映选择性α-胺化反应。所需的α-酰肼酯以优异的收率和高对映体过量得到，从而在广泛的底物范围内得到具有季立体中心的产物。
