新型抗抑郁药阿戈美拉汀的合成工艺研究  

Improved Synthetic Methods of Antidepressant Agomelatine

作　　者：王波 郭杰 梁伟 伍忆 孙洁华 朱姣 柳静 Wang Bo;Guo Jie;Liang Wei;Wu Yi;Sun Jiehua;Zhu Jiao;Liu Jing(Research and Development Department,Hunan Dongting Pharmaceutical Company,Changde 415001,China)

机构地区：[1]湖南洞庭药业股份有限公司技术总部,湖南常德415001

出　　处：《广东化工》2023年第1期56-58,共3页Guangdong Chemical Industry

摘　　要：本研究解决当前工艺安全风险高、收率低的问题,以市售化学品(7-甲氧基-1-萘基)乙腈为原料,经三氯化铝条件下使用四氢铝锂还原,然后再经氨化得到(7-甲氧基-1-萘基)乙胺,然后经乙酰化、精制得到阿戈美拉汀,总收率85%~90%,纯度大于99.6%。考察了温度、碱液浓度对反应的影响,结果表明-5~5℃为中间体制备的最佳温度范围,40%的氢氧化钠处理是收率、质量以及安全性的最优条件。研究改进了工艺过程,研究了除杂工艺和后处理方式。Disclosed is a process of lower safety risk and higher yield for the synthesis of the new antidepressant agomelatine.Synthesized from key starting material 7-Methoxy-1-naphthyacetonitrile.Reduction with LiAlH4and AlCl3.The target compound is obtained in 85%~90%overall yield and more than 99.6%purity after ammoniation,acetylization and recrystallization.The study relates to the infection of reaction temperature and the density of sodium hydroxide solution,which shows that within-5~5℃and 40%density is the best condition.The studies also include improved after treatment,impurities removing and scalable process.

关 键 词：阿戈美拉汀 抗抑郁药 (7-甲氧基-1-萘基)乙腈 三氯化铝 四氢铝锂 

分 类 号：TQ463.42[化学工程—制药化工]