Abstract

The crucial intermediate A with a racemization barrier of 16 kcal mol−1 at −78 °C is proposed for the asymmetric α-methylation of 1 to give 2 in 81 % ee and 96 % yield (see scheme). The asymmetric α-methylation occurs in other amino acid derivatives (Dopa, Val, Leu, Trp, His, Tyr) in 78–93 % ee.

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