Abstract
Unnatural α-amino acids play important roles in peptide-based drugs and isosteres. The preparation of unnatural amino acids in high stereochemical purity is a challenging and important task. In the present work, β-substituted bisphosphonates are explored as Michael acceptors. Utilizing azomethine ylid nucleophiles, unnatural α-amino acids containing two adjacent tertiary stereogenic centers are produced in excellent yield, diastereoselectivity, and enantioselectivity.
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