甲磺酸多沙唑嗪合成工艺研究

Study on Synthesis of Doxazosin Mesylate

以邻苯二酚与环氧氯丙烷为原料,经环合、氧化、氯化、酰化、缩合、成盐等反应合成了治疗高血压和良性前列腺增生的药物甲磺酸多沙唑嗪。原料廉价,易得,反应条件温和,操作方便。

Doxazosin mcsylate used in the therapy of hypertension and benign prostatic hyperplasia was synthesized from catechol by cyclization, oxidation, chlorination, aminatio and condensation to give doxazosin followed by salt formation with methane sulfonic acid with an overall yield of 19.4 %. The reaction conditions are mild and the raw materials are commercially available.