Preparation of highly substituted γ-lactam follicle stimulating hormone receptor agonists

An unusual combination of Weinreb amidation and Mitsunobu lactam formation was used to prepare highly substituted γ-lactam analogues of a thiazolidinone follicle stimulating hormone receptor agonist. The analogue synthesis was stereoselective and the final products were chemically stable. Biological properties of the target molecules were nearly identical to those of the lead compound.

Preparation and testing of the highly substituted γ-lactam analogues 2 is reported.Figure optionsDownload as PowerPoint slide