Acetic acid, azido-, ethyl ester → Ethyl 2-(5-(1-(5-acetamido-2',4'-difluoro-[1,1'-biphenyl]-3-yl)-1H-benzo[d]-imidazol-5-yl)-1H-1,2,3-triazol-1-yl)acetate

関与物質

反応手順

A mixture of N-(5-(5-ethynyl-1H-benzo[d]imidazol-1-yl)-2′,4′-difluorobiphenyl-3-yl)acetamide (258 mg, 0.6 mmol), ethyl-2-azidoacetate (180 mg, 0.8 mmol, 1.3 eq.), sodium ascorbate (125 mg, 0.6 mmol, 1.0 eq.) and copper sulfate pentahydrate (80 mg, 0.32 mmol, 0.5 eq.) in t-butanol and water (1:1, 3 ml) was stirred for 12 h at RT. The mixture was quenched with water and the precipitate formed was filtered and dried to give the product in 75% yield (250 mg).

情報源と証拠