雷诺嗪的合成工艺研究

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.

Study on Synthesis Process of Ranolazine

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 such as reagents and temperature were optimized as well.The overall yield is up to 70.1%.The structure of the target product is confirmed by MS,IR,1H-NMR.The proposed synthetic method could be a choice for industrial production of ranolazine,due to its simple procedure,low production cost and low pollution.