反应详情

Methyl 4-(4-chloro-1H-imidazol-1-yl)-3-methoxyphenylcarbamimidothioate, hydroiodide (4.0 g, 13.48 mmol, from preparation A) and 6-chloro-2-(4-fluorophenyl)hexanoic acid (3.63 g, 14.83 mmol, from preparation AC) were coupled and then reacted with hydrazine (1.69 mL, 53.9 mmol) using a procedure analogous to Step A of Example 13 to afford 5-(5-chloro-1-(4-fluorophenyl)pentyl)-N-(4-(4-chloro-1H-imidazol-1-yl)-3-methoxyphenyl)-1H-1,2,4-triazol-3-amine (5.2 g, 10.63 mmol, 79% yield) as a reddish foam solid. LC-MS (M+H)+ 489.1. Used the crude isolate in the next step without purification.