Promiscuous Candida antarctica lipase B-catalyzed synthesis of β-amino esters via aza-Michael addition of amines to acrylates

An efficient protocol for the regioselective aza-Michael addition of amines with acrylates using CaLB as a biocatalyst at 60 C has been developed The reaction is applicable to a wide variety of primary and secondary amines with different acrylates to synthesize the corresponding B-ammo esters with good yields An alternative route for the synthesis of higher beta-amino esters through the additional transesterification step is also studied and was found effective (C) 2010 Elsevier I.td All rights reserved