甲磺酸多沙唑嗪合成工艺研究

Study on Synthesis of Doxazosin Mesylate

以1,4-苯并二噁烷-2-羧酸为起始原料,经胺化、缩合、解离、成盐得到甲磺酸多沙唑嗪。通过单因素实验考察了合成过程中摩尔比、反应温度、反应时间等工艺参数对反应的影响。最终产品经1H-NMR、13CNMR、MS确证结构是正确的,纯度>99%,总收率为78.0%,合成工艺简单,适于工业化生产。

Doxazosin mesylate is obtained through amination,condensation,dissociation,and salt formationwith 1,4-benzodioxane-2-carboxylic acid as the starting material.The influence of themolar ratio,reaction temperature,reaction time,and other process parameters on the reaction during the synthesis process was investigatedby single factor experiments.The structure of doxazosin mesylate was confirmed by 1H-NMR,13C-NMR and MS,with a purity of>99%,and a total yield of 78.0%.The synthesis process is simple and suitable for industrial production.