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目的设计合成甲氧苄啶(TMP)的2个重要杂质TMP-A和TMP-F。方法以3,4,5-三甲氧基苯甲醛为原料,经过缩合、重排、加成、环合、氯代及亲核取代制得TMP-A。以香兰素为原料,经过缩合、重排、加成和环合制得TMP-F。结果与结论成功制备了TMP-A,收率较文献提高。首次合成TMP-F,所设计路线的反应条件温和,试剂廉价易得,操作简单。
Objective To design TMP-A and TMP-F, two important impurities of synthetic trimethoprim (TMP). Methods TMP-A was prepared from 3,4,5-trimethoxybenzaldehyde by condensation, rearrangement, addition, cyclization, chlorination and nucleophilic substitution. With vanillin as raw material, after condensation, rearrangement, addition and cyclization TMP-F. RESULTS AND CONCLUSION TMP-A was successfully prepared and the yield was improved compared with the literature. For the first time, TMP-F was synthesized and the reaction conditions of the designed route were mild. The reagents were cheap and easy to operate, and the operation was simple.