Enantioselective Biginelli Reaction
Posted by naturalproductman on June 30, 2009
Hee-Yoon Lee at KAIST has recently published in the European Journal of Organic Chemistry on a proline ester salt catalyzed asymmetric Biginelli reaction, which involves the coupling of an aryl aldehyde, urea, and a beta-ketoester to form a 3,4-dihydropyrimidin-2(1H)-one
(DHPM). They used a t-butoxy proline ester (20 mol%) for optimal enantioselectivity (71:29).