O-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate → 2-(4-(4-Fluoro-3-methyl-phenyl)-2-phenyl-imidazol-1-yl)-1-(2-methyl-4,5,7,8-tetrahydro-thiazolo[4,5-d]azepin-6-yl)-ethanone

Participants

Reaction Steps

45 mg 2-methyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepine hydrochloride was added to 60 mg (4-(4-fluoro-3-methyl-phenyl)-2-phenyl-imidazol-1-yl)-acetic acid, 70 mg TBTU, 0.06 mL TEA in 1 mL DMF. The reaction was stirred over night at RT. The mixture was purified by HPLC (ZORBAX StableBond C18; 5 μm; 30×100 mm; gradient: water (+0.3% formic acid)/acetonitril=90/10-10/90 in 9 min; flow: 50 ml/min.) to give 20 mg desired product. Rt: 0.94 (method A), (M+H)+: 461

Provenance & Evidence