Synthesis of conformationally constrained α-amino acid derivatives containing bicyclo[2.2.2] unit via the Diels-Alder and Suzuki-Miyaura cross-coupling reactions as key steps

A simple route to synthesize conformationally constrained a-amino acid (AAA) derivatives containing bicyclo[2.2.2]octane ring-system has been devised. Diels-Alder reaction is chosen to assemble highly constrained AAA derivatives and the scope of the methodology is further expanded by Suzuki-Miyaura cross-coupling reaction with various boronic acids.