雷诺嗪的合成工艺研究
Study on Synthesis Process of Ranolazine
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摘要: 以2,6-二甲基苯胺为起始原料,以哌嗪单盐酸盐替代哌嗪,经五步反应合成雷诺嗪.从试剂和操作温度等方面优化了各步的反应条件,总收率70.1%,目标产物的结构经MS、IR、1H-NMR确证.此合成路线工艺简单,原料价廉,副产物得到回收利用,污染小,可为工业化生产的实施提供参考.Abstract: Ranolazine is a novel anti-angina drug with brightly applicable prospect,but obstacles for the application of ranolazine include hard operation conditions,high piperazine consumption and low yield,etc.in the syntheses reported in literatures.Ranolazine was synthesized with 2,6-dimethyl aniline as starting precursor.Monohydrochloride piperazine was used instead of piperazine for the synthesis of N-(2,6-dimethylbenzyl)-1-piperazinylacetamine,resulting in decreased piperazine consumption.Reaction conditions su...