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The formation and 2-amino alcohol catalyzed addition of arylzinc reagents from and with boronic acids, respectively, is drastically accelerated to a few minutes under microwave irradiation without loss of enantioselectivity (up to 98% ee). Of the amino acid derived catalysts tested, the conformationally restricted bulky substituted aziridine-2-methanols derived from serine show the best overall performance in the formation of diarylmethanols.
Publications
A simple, rapid, one-pot multicomponent synthesis of tryptophan-derived diketopiperazines with variable side chains is presented. Microwave radiation gives comparable yields, but allows a significant decrease in reaction times.