A modular, general and enantiospecific strategy for the synthesis of CVS 1778 analogs: inhibitors of factor Xa

A modular synthetic route has been developed for the synthesis of a series of complex benzalactams which are potent inhibitors of factor Xa. The route produces fused benzalactams of varying ring size via a key-step ring-closing metathesis reaction. The route also facilitates the synthesis of discrete enantiomers using readily available commercial building blocks.