目的 合成拉喹莫德并對工藝進行研究。方法 以2-氨基-6-氯苯甲酸為起始原料，經(jīng)成環(huán)反應(yīng)、甲基化反應(yīng)、縮合反應(yīng)、水解反應(yīng)等合成了拉喹莫德。結(jié)果 合成的拉喹莫德總收率為71.8%。結(jié)論 工藝改進后，簡化了操作過程，提高了拉喹莫德的收率。

Objective To synthesize Laquinimod and improve the synthetic technology. Methods Taking 2-amino-6- chlorobenzoic acid as the raw material, Laquinimod was obtained after a series of chemical reactions including cyclization, methylation, condensation, and hydrolization reaction. Results Laquinimod was prepared with an overall yield rate of 71.8%. Conclusion The improved procedure could simplify the synthesis and increase the yield of Laquinimod.

科技部“十二五”重大新藥創(chuàng)制（2011ZX09102-007-03）；廣東省教育廳高層次人才資助項目；廣東省科技計劃項目（2010B030700044，2011A030100013）