Abstract

Abstract O,O-Dialkyl 1-benzylaminobenzylphosphonates (3) formed in quantitative yield at R.T. by the nucleophilic addition of dialkyl phosphite (1) to benzylidenebenzylamines (2) in CH2C12 give highly characteristic fragmentation patterns in their positive ion FAB mass spectrum. Catalytic hydrogenolysis of these precursors produces ‘P1’ structural units which when incorporated into substrate-like peptides, form potent inhibitors of thrombin.

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