替米沙坦合成技术研究进展

Research Progress on the Synthesis of Telmisartan

替米沙坦(telmisartan)因其高度受体亲合力,优越的药代动力学以及长效高效的特性,已逐渐成为抗高血压的首选药物。但目前存在其工艺合成路线长、反应条件苛刻、后处理复杂、收率低等一系列问题。对国内外文献中替米沙坦的主流合成技术进行了综述,分别介绍了以甲苯衍生物和苯并咪唑类衍生物为起始原料合成替米沙坦的合成路线,讨论了各条合成路线在原料选择、反应条件、反应步骤等方面的优缺点。提出了比较适合工业化大规模生产的合成路线。

Telmisartan has gradually become the first choice of antihypertensive drugs because of its high affinity for receptor,superior pharmacokinetics and long-lasting efficient properties.However,there are a series of problems,such as long synthesis route,strict reaction conditions,complicated post-processing,low yield and so on.The main synthesis technology of telmisartan in domestic and foreign literatures was reviewed.The synthesis routes of telmisartan using benzene and toluene derivatives and imidazoles derivatives,as starting materials were introduced.For each route the selection of raw material,the advantages and disadvantages of reaction conditions and reaction steps and etc were discussed.The synthetic route suitable for industrial mass production was proposed.