【摘要】 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A1Cl3)=1∶1.3:反应时间5 h;反应温度165~170℃时,环合反应收率达83.1%。更多还原

【Abstract】 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 who1e course ran smoothly.The overall yield reached 58.8%.Experimental results indicated,the acetamide(Ⅲ)and aluminium chloride in mo1e ratio 1∶1.3 reacted at 165～170℃ for(5 h) to give the cyclization product in 83.1% yield.更多还原