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Squaramide-catalysed enantionselective Mannich reaction of imines bearing a heterocycle with malonates†
Hai-Xiao He,Da-Ming Du
RSC Advances Pub Date : 07/08/2013 00:00:00 , DOI:10.1039/C3RA43260B
Abstract

An efficient enantioselective Mannich reaction of imines bearing a heterocycle with malonates catalysed by a cinchona-based squaramide organocatalyst has been developed. This catalytic asymmetric reaction afforded the β-amino ester derivatives containing a heterocycle moiety in high yields (up to 99%) and excellent enantioselectivities (up to 98%) in most cases. The imines with an electron-withdrawing group afforded the adducts with better yields than those bearing an electron-donating group in this reaction.

Graphical abstract: Squaramide-catalysed enantionselective Mannich reaction of imines bearing a heterocycle with malonates
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