SYNTHESIS AND STRUCTURE OF CIS-PEPTIDYL PROLINAMIDE MIMETICS BASED UPON 1,2,5-TRIAZEPINE-3,6-DIONES

The synthesis of novel constrained cis-peptidyl prolinamide mimetics f or the dipeptide amides glycyl (2S)-prolinamide, (2S)-alanyl (2S)-prol inamide and (2R)-alanyl (2S)-prolinamide and some analogues, based upo n fused 1,2,5-triazepine-3,6-diones, is described; these are suitable for elaboration into larger peptides at both the carboxy and amino ter mini, X-ray crystal structures for some of the compounds and intermedi ates are also presented.