摘要
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.
出处
《海峡药学》
2017年第5期247-249,共3页
Strait Pharmaceutical Journal
基金
国家重大新药创制专项创新抗耐药抗生素研制及重大品种的综合技术提升课题(编号:2014ZX09201001)