The 1,4-benzodiazepine-2,5-dione template has found widespread therapeutic use across a range of disease states. The closely related 1,4-benzodiazepin-2-one nucleus is less utilised yet has demonstrated anticonvulsant, 1 anti-HIV 2 and anti-coagulant 3 activity. We wished to access a diverse range of these compounds for testing throughout a number of discovery programmes. Two solid phase approaches have been disclosed, 4., and and although ...