Solution and solid phase synthetic methods leading to the rapid, stere
ocontrolled construction of highly functionalized fused bicyclic amino
acid derivatives have been developed. The key step involves a unique
application of the intramolecular Pauson-Khand cyclization for the con
struction of hexahydro-1H-[2]pyrindinone ring systems. Further modific
ations which demonstrate the potential for combinatorial library gener
ation are also disclosed. (C) 1997 Published by Elsevier Science Ltd.