Natural products as templates for bioactive compound libraries: synthesis of biaryl derivatives of (+/-)-vasicine.

A reliable and high-yielding procedure for preparation of 7-aryl and 7-heteroaryl derivatives of (+/-)-vasicine in two steps from the naturally occurring material is described. This protocol broadens the chemical space for selective modifications of the vasicine tricyclic structure, thereby making it a valuable starting point for the development of novel compound libraries with potentially beneficial biological profiles.