氯美昔布的合成研究

Study on the Synthesis of Lumiracoxib

以对甲苯胺为起始原料，经氯乙酰化，2-氯-6-氟苯酚醚化、重排，再经氯乙酰化，无水AlCl3催化下环合，最后经开环反应制得氯美昔布，整个反应条件温和，反应总收率达到58．8％。在环合反应中，n（Ⅲ）：n（无水AlCl3）=1：1．3：反应时间5h；反应温度165—170℃时，环合反应收率达83．1％。

Lumiracoxib was synthesized by chloroacetylation of p - Toluidine with chloroacetyl chloride, etherincation with 2 - chloro- 6 - fluorophenol and rearragement reaction, then chloroacetylation again, cyclization catalyzed by anhydrous aluminium chloride,and ring opening reaction.The whole course ran smoothly. The overall yield reached 58.8% .Experimental results indicated,the acetamide（ Ⅲ ）and aluminium chloride in mole ratio 1：1.3 reacted at 165 ～ 170℃ for 5 h to give the cyclization product in 83.1% yield.