Sheng Chun
2002
Citations
0
Influential Citations
1
Citations
Journal
Chinese Journal of Medicinal Chemistry
Abstract
The optimization of the synthesis of 1 [2 (2,4 difluorophenyl) 2,3 epoxypropyl] 1 H 1,2,4 triazole methanesulphonate,which is the key intermediate of the fluconazole by the orthogonal experimental design was reported.A mixture of 2′,4′ difluoro 2 (1 H 1,2,4 triazole 1 yl) acetophenone(29 8 g,0 115 mol),trimethylsulfoxonium iodide(25 3 g,0 115 mol) and cetyltrimethylammonium bromide(1 6 g) was stirred in 180 mL of toluene together with 75 mL of 20% w/w of aqueous sodium hydroxide at 60℃ for a period of 3 h.The yield was 62 34%.The new method has several advantages such as the cheap reactants,facile reaction conditions,convenient operation and high yield.