Solid Phase Synthesis of 3,4,7-Trisubstituted 4,5,8,9-Tetrahydro-3H-imidazo[1,2-a][1,3,5]triazepin-2(7H)-thiones and N-Alkyl-4,5,7,8-tetrahydro-3H-imidazo[1,2-a][1,3,5]triazepin-2-amines

摘要: The solid-phase parallel synthesis of 3,4,7-trisubstituted 4,5,8,9-tetrahydro-3H-imidazo[1,2-a][1,3,5]triazepin-2(7H)-thiones and N-alkyl-4,5,7,8-tetrahydro-3H-imidazo[1,2-a][1,3,5]triazepin-2-amines starting from resin-bound dipeptides is described. key synthetic steps involve the cylization an amino a guanidino functionality using thiocarbonyldiimidazole subsequent transformation resulting thiourea moiety to substituted guanidine group HgCl(2) various amines. Following cleavage resin, desired products were obtained in good yields moderate purities, depending on building blocks employed.