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4-甲磺酰基苯乙酸成锂盐后与6-甲基吡啶-3-羧酸甲酯偶联得1-(6-甲基吡啶-3-基)-2-[4-(甲磺酰基)苯基]乙酮,与(2-氯-3-二甲胺基-亚-2-丙烯基)-二甲基-铵六氟磷酸盐关环得粗品依托考昔,粗品与对甲苯磺酸成盐后游离得纯度99.8%的COX-2抑制剂依托考昔,总收率54%。
Methyl 4-methanesulfonyl phenylacetate was coupled with methyl 6-methylpyridine-3-carboxylate to give 1- (6-methylpyridin-3-yl) -2- [4- ) Phenyl] ethanone and the crude product of ethacryl and (2-chloro-3-dimethylamino-propen-2-propenyl) -dimethyl-ammonium hexafluorophosphate, Acid salt free free purity of 99.8% of COX-2 inhibitor etocopyoxel, the total yield of 54%.