Celecoxib的合成

Synthesis of Celecoxib

以对甲基苯乙酮、三氟乙酸乙酯等为原料合成中间体 1- (4-甲基苯基 ) - 4,4,4-三氟 - 1,3-丁二酮 ,再与对肼基苯磺酰胺盐酸盐进行脱水环合即得 celecoxib,总收率 48.3%。

The condensation of 4' methylacetophenone with ethyl trifluoroacetate by means of Na in methanol gives 1 (4 methylphenyl) 4,4,4 trifluorobutane 1,3 dione, which is cyclized with (4 sulfamoylphenyl) hydrazine hydrochloride to give celecoxib in overall yield of 48.3%.