盐酸米诺环素合成工艺研究

Study on the Synthesis of Minocycline Hydrochloride

目的优化抗感染药物和关键中间体盐酸米诺环素的合成工艺。方法以盐酸去甲基金霉素为原料通过还原、碘代和Stille偶联反应得到目标产物。结果目标产物经过核磁共振氢谱和质谱确认化学结构,总收率为40%,纯度为98.5%。结论经过该合成工艺操作简单,产品纯度高,且易于实现工业化。

OBJECTIVE To optimize the synthesis of minocycline hydrochloride, an anti-infective drug and the key intermediate. METHODS Minocyeline hydrochloride was synthesized by using demeeloeycline hydrochloride as a starting material through reduction, iodination and stille coupling reaction. RESULTS Minocyeline hydrochloride was characterized by IHNMR and MS, The total yield was 40% and the purity was 98.5%. CONCLUSION The suitable synthesis process of minocycline hydrochloride with high purity, easy operation and amendable to industriali- zation was provided.