Potassium Iodide → 1-[2-(4-{2-[(e)-2-(4-Trifluoromethyl-phenyl)-vinyl]-thiazol-4-ylmethoxy}-phenyl)-thiazole-4-ylmethyl]-1h-[1,2,3]triazole

関与物質

反応条件

反応手順

A mixture of 0.129 g (0.50 mmol) 4-(4-[1,2,3]triazol-1-ylmethyl-thiazol-2-yl)-phenol and 0.10 g (0.30 mmol) cesium carbonate in 10 ml butanone was stirred at 60° C. for 30 min, then 0.153 g (0.50 mmol) 4-chloromethyl-2-[2-(4-trifluoromethyl-phenyl)-vinyl]-thiazole and 0.083 g (0.50 mmol) potassium iodide were added and stirring at 60° C. continued over night. After evaporation, 15 ml water was added and the mixture extracted with two portions of 15 ml ethyl acetate. The combined organic layers were washed with 1N sodium hydroxide and water, dried over sodium sulfate and evaporated to give 174 mg raw material which was purified on silica. Elution with ethyl acetate/heptane 5:1 yielded 86 mg white crystals (33%) of 1-[2-(4-{2-[2-((E)-4-trifluoromethyl-phenyl)-vinyl]-thiazol-4-ylmethoxy}-phenyl)-thiazol-4-ylmethyl]-1H-[1,2,3]triazole melting at 146-148° C.

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