依地昔布关键中间体的合成及表征

Synthesis and Characterization of Key Intermediate of Etoricoxib

以茴香硫醚为原料,经傅克酰基化、氧化、Willgerodt-Kindler重排羧酸化法、Claisen缩合四步反应合成高选择性环氧化醚-2(COX-2)抑制剂依地昔布关键中间体2-(4-甲砜基苯基)-1-(6-甲基-3-吡啶基)乙酮,四步合成总收率39.0%,HPLC纯度92.3%,精制后HPLC纯度98.2%。对其中关键产物对甲砜基苯乙酸和2-(4-甲砜基苯基)-1-(6-甲基-3-吡啶基)

2-（4-carbosulfonylphenyl）-1-（6-methyl-3-pyridinyl）ethanone,a key intermediate of Etoricoxib,was synthesized from thioanisole via Friedel-Crafts acylation,Oxidation,Willgerodt-Kindler rearrangement,Claisen condensation with an overall yield of 39% and HPLC purity of 92.3% with further purification.4-（Methanesulfonyl）phenylacetic acid and 2-（4-Mesylphenyl）-1-（6-methylpyridin-3-yl）-ethan-1-one as key products were characterized with IR and NMR.