Journal of the American Chemical Society, Vol.132, No.44, 15474-15476, 2010
Asymmetric Bromolactonization Using Amino-thiocarbamate Catalyst
A novel amino-thiocarbamate-catalyzed bromolactonization of unsaturated carboxylic acids has been developed. The scope of the reaction is evidenced by 22 examples of gamma-lactones with up to 99% yield and 93% ee. The protocol was applied in the enantioselective synthesis of the key intermediates of VLA-4 antagonists.