强效降眼内压药—安普乐定的合成方法探讨

Research on the synthesis of potent decreasing IOP drug Apraclonidine

目的 探讨安普乐定的合成方法。方法 采用对硝基苯胺为原料,经还原、加保护基、甲酰化、氯化、环合、脱保护基六步反应法可进行化学合成。结果及结论 该合成方法所需试剂安全易得,合成条件平和,适于工业化生产。

Objective To research the synthesis method of Apraclonidine. Methods Apraclonidine was synthesized from P-Nitraniline by reaction with reduction, adding protection group, formylation, chlorination, cyclization, off-protecting group. Results andconclusion The raw materials were safe and cheap. The reaction conditions were mild. Therefore the industrialization of productioncould be achieved by this method.