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[1]王凯,符兆林,王林元,等.盐酸利托君合成新工艺[J].武汉工程大学学报,2008,(04):31-32.
　WANG Kai,FU Zhao lin,WANG Lin yuan,et al.New synthetic route of ritodrine hydrochloride[J].Journal of Wuhan Institute of Technology,2008,(04):31-32.
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《武汉工程大学学报》[ISSN:1674-2869/CN:42-1779/TQ]

卷:
期数:
2008年04期
页码:
31-32
栏目:
化学与化学工程
出版日期:
2008-04-30

文章信息/Info

Title:
New synthetic route of ritodrine hydrochloride
文章编号:
16742869(2008)04003102
作者:
王凯; 符兆林; 王林元; 张秀兰; 葛艳丽; 巨修练*
湖北省新型反应器与绿色化学工艺重点实验室，武汉工程大学化工与制药学院，湖北 武汉 430074
Author(s):
WANG Kai;  FU Zhaolin;  WANG Linyuan;  ZHANG Xiulan;  GE Yanli;  JU Xiulian
School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology,
Hubei Key Lab of Novel Reactor and Green Chemical Technology, Wuhan 430074, China
关键词:
利托君; 对羟基苯丙酮; 新工艺
Keywords:
ritodrine; pHydroxyphenylacetone; new technology
分类号:
TQ460.31
DOI:
-
文献标志码:
A
摘要:
对盐酸利托君的合成路线进行了改进研究，减少酚羟基的保护和脱保护步骤，并对反应条件和过程控制进行优化.以对羟基苯丙酮为起始原料，经溴化、缩合成盐、Pd/C催化加氢还原得到目标产物盐酸利托君，总收率389%，并对其结构进行质谱、红外和元素分析的确证.结果显示该路线是可行的，操作过程简单，产品收率较高，能较好满足工业化大生产要求.
Abstract:
Synthetic route of ritodrine hydrochloride was innovated. The reaction steps of increasing phenol group protection and removing its protection were reduced, and the reaction conditions and processing control were optimized. With phydroxyphenylacetone as the beginning material, Ritodrine hydrochloride was prepared by the reaction of bromination, condensation with pmethoxyphenylethylamine, salt reaction and hydrogenation with adding hydrogen and Pd/C catalyst. The total yield was 38.9% and its structure was confirmed by MS, IR and elemental analysis. The results showed that the route is feasible, the operation is simple, and the product yield is higher. New synthetic route can meet the demands of large industrialized production.

参考文献/References:

［1］Hamada Y， Nakaya Y， Hamada S， et al. Activation of K+ channels by ritodrine hydrochloride in uterine smooth muscle cells from pregnant women［J］. Euro J Pharma: Molecular Pharmacology, 1994, 28 (1)：4551.
［2］Hosakere D R, Bochhegowda M. Spectrophotometric methods for the determination of ritodrine hydrochloride and its application to pharmaceutical preparations［J］.2001, 56(8)：615619.
［3］任进知，叶晓镭，江天维. 利托君的合成新路线［J］.中国医药工业杂志，2000，31（6）：241242.
［4］胡厚才. 对羟基苯乙酮和覆盆子酮制备莱克多巴胺的新方法：中国，1557804A［P］. 20041209.
［5］Naoki Y， Yoshimasa F， Yoshiaki S， et al. ()ritodrine, therapeutic compositions and use, and method of preparation：US，5449694 ［P］. 1995912.

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备注/Memo

备注/Memo:
收稿日期：20070409
作者简介：王凯(1976)，男，湖北武汉人，讲师.
研究方向：医药产品研发、中试放大、工艺革新和药品申报.
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