喹硫平关键中间体的合成工艺优化  

Optimization of Synthesis of Key Intermediate of Quetiapine

作　　者：柳静 孙洁华 吴南林 Liu Jing;Sun Jiehua;Wu Nanlin(Hunan Dongting Pharmaceutical Co.,Ltd.,Changde 415001,China)

机构地区：[1]湖南洞庭药业股份有限公司,湖南常德415001

出　　处：《广东化工》2021年第13期57-58,共2页Guangdong Chemical Industry

摘　　要：本研究优化了喹硫平关键中间体氯化物(11-氯二苯并[b,f][1,4]硫氮杂?)的合成工艺,以10H-二苯并[b,f][1,4]硫氮杂?-11-酮和三氯氧磷为原料,甲苯为溶剂,N,N-二甲基苯胺为催化剂,经过氯化反应得到目标产物氯化物,后续制成喹硫平,收率可达90%,纯度大于99.5%。本工艺优化三氯氧磷的投料量,大幅提高了产品收率,为后期的含磷废水处理减轻了压力,适合工业化生产。In this paper, the synthesis process of quetiapine key intermediate chloride(11-chlorodibenzo [b, f] [1,4] thiazapine) was optimized.10 H dibenzo [b, f] [1,4] thiaaza-11-one and phosphorus oxychloride were used as raw materials, toluene as solvent and N, N-dimethylaniline as catalyst, The target product chloride was obtained by chlorination reaction. The yield and purity of quetiapine were 90 % and 99.5 %, respectively. The process optimizes the feeding amount of phosphorus oxychloride, greatly improves the product yield, reduces the pressure for the later treatment of phosphorus containing wastewater, and is suitable for industrial production.

关 键 词：喹硫平 中间体 氯化反应 合成 条件优化 

分 类 号：TQ[化学工程]