Palladium-catalyzed borylation and Suzuki coupling (BSC) to obtain beta-substituted dehydroamino acid derivatives

Abstract

Several benzo[b]thienyldehydroamino acids were prepared by one pot palladium-catalyzed borylation and Suzuki coupling (BSC) from bromobenzo[b]thiophenes containing EDG (OMe or Me), as the component to be borylated with pinacolborane, and pure stereoisomers of beta-bromodehydroamino acid derivatives. To our knowledge it is the first time that the BSC reaction involves a non aromatic system.