Asymmetric Aza-Mannich Addition: Synthesis of Modified Chiral 2-(Ethylthio)-thiazolone Derivatives with Anticancer Potency

An easily prepared cinchona alkaloid derivative was found to be an effective organocatalyst in a direct, enantioselective aza-Mannich addition. By establishing a quaternary carbon stereocenter, a series of modified chiral 2-(ethylthio)-thiazolone derivatives have been obtained with excellent diastereo- and enantioselectivities. And these derivatives have been found to show anticancer activities against five different cancer cell lines using the MTT assay.