Rapid entry into the cryptohycin core via an acyl-#beta#-lactam macrolactonization:total synthesis of cryptophycin-24

摘要

An efficient,concise approach to the macrolide core of te cryptophycins,potent antimitotic agents,has been achieved.The reaction sequence features a novel macrolactonization utilizing a reactive acyl-#beta#-lactam intermediate that incorporates the #beta#-amino acid moiety within the 16-membered macrolide core.This highly modular approach,which allows for multiple alterations thrughout the structure,was successfully applied to the total synthesis of cryptophycin-24.