Synthesis of conformationally constrained alpha-imino acid derivatives via ring-closing metathesis

摘要

Conformationally constrained amino acid derivatives are useful in the synthesis of peptidomimetics. Seven-, and eight-membered conformationally constrained alpha-imino acid derivatives have been prepared via RCM (ring-closing metathesis). Interestingly, attempts to achieve the synthesis of nine-membered imino acid derivative resulted in the formation of dimeric, 18-membered macrocyclic bis-alpha-imino acid derivative.