4-[（2-甲基-4-喹啉基）-甲氧基]苯甲酸合成工艺研究

目的：改进β-苯甲酰氨基类肿瘤坏死因子转化酶（TACE）抑制剂重要中间体4-（2-甲基-4-喹啉基）-甲氧基]苯甲酸的合成工艺。方法：以2-甲基喹啉为起始原料,经过羟甲基化、氯代、威廉姆森成醚反应、水解得到目标化合物。结果与讨论：目标化合物和中间体的结构经1HNMR和FAB-MS确证。该路线优化了合成工艺,收率高,原料易得,成本低廉,操作简单,总收率约为47.5%。

Synthesis of 4-[(2-methylquinolin-4-yl)methoxy] benzoic acid

Objective： To improve the synthetic route and synthesize 4- （2-methylquinolin-4-yl ] methoxy ） benzoic acid, which is a key intermediate for the synthesis of β-benzamido TACE inhibitors. Methods：The target compound was synthesized from 2-methylquinoline by hydroxymethylation, chlorination, etherification and hydrolysis. Result and Conclusion：The ^1H-NMR and MS data of the intermediates and the target compound were identical with those reported in literature. With this improved route the total yield is 47.5%. This improved synthetic route is convenient, efficient and cost-effective.