科研之友
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摘要
A method for the asymmetric synthesis of enantioenriched anti-alpha-hydroxy-beta-amino acid derivatives by enantioconvergent reduction of the corresponding racemic alpha-keto esters is presented. The requisite alpha-keto esters are prepared via Mannich addition of ethyl diazoacetate to imines followed by oxidation of the diazo group with Ozone. Implementation of a recently developed dynamic kinetic resolution of beta-substituted-alpha-keto esters via Ru(II)-catalyzed asymmetric transfer hydrogenation provides the title motif in routinely high diastereo- and enantioselectivity.
- 出版日期2013-5-17
