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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 drug of choice for antihypertensive drug because of its high affinity to the receptor, superior pharmacokinetics, and long-acting and high-potency properties. However, there are a series of problems such as long process route, harsh reaction conditions, complicated post-treatment and low yield. The main synthesis methods of telmisartan in domestic and foreign literature were reviewed. The synthesis routes of telmisartan with toluene derivatives and benzimidazole derivatives as starting materials were introduced respectively. The synthesis routes of telmisartan were discussed. In the choice of raw materials, reaction conditions, reaction steps and other aspects of the advantages and disadvantages. Proposed a more suitable for large-scale industrial production of synthetic routes.