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A highly diastereoselective Friedel–Crafts reaction of indoles with isatin-derived N-sulfinyl ketimines towards the efficient synthesis of chiral tetrasubstituted 3-indolyl-3-aminooxindoles†
Jian-Ping Chen,Wen-Wen Chen,Yi Li,Ming-Hua Xu
Organic & Biomolecular Chemistry Pub Date : 01/29/2015 00:00:00 , DOI:10.1039/C5OB00063G
Abstract

A Lewis acid promoted highly diastereoselective asymmetric Friedel–Crafts alkylation of indoles with isatin-derived N-tert-butanesulfinyl ketimines is described. The reaction can be accomplished with ease in the presence of a catalytic amount of Bi(OTf)3, providing a series of 3-indolyl-3-aminooxindoles in excellent diastereoselectivities (up to 98% de) and yields (up to 99%).

Graphical abstract: A highly diastereoselective Friedel–Crafts reaction of indoles with isatin-derived N-sulfinyl ketimines towards the efficient synthesis of chiral tetrasubstituted 3-indolyl-3-aminooxindoles
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