反应详情

Methyl 4-(4-(difluoromethyl)-1H-imidazol-1-yl)-3-methoxyphenylcarbamimidothioate hydroiodide (500 mg, 1.601 mmol, from preparation N) and 6-chloro-2-(4-fluorophenyl)hexanoic acid (392 mg, 1.601 mmol, from preparation AH) were coupled and then reacted with hydrazine (0.201 mL, 6.40 mmol) using a procedure analogous to Step A of Example 13 to afford 5-(5-chloro-1-(4-fluorophenyl)pentyl)-N-(4-(4-(difluoromethyl)-1H-imidazol-1-yl)-3-methoxyphenyl)-1H-1,2,4-triazol-3-amine (821 mg, 100% yield). LC-MS (M+H)+ 505.3. The crude products were used in the subsequent step without purification.