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发明公开
CN101774986A 一种制备阿利克伦及其中间体的方法 有权

一种制备阿利克伦及其中间体的方法
摘要：
本发明涉及一种制备阿利克伦及其中间体的方法，属于药物制备方法技术领域，本方法是将4-溴-1-甲氧基-2-(3-甲氧基丙氧基)苯与异丙基氯化镁和正丁基锂反应制得式XXII化合物与式XIX化合物经甲磺酰化后与无水溴化锂反应制得的式XXI化合物在醚类溶剂中有含铁的催化剂存在下，制备得式XV所示阿利克伦中间体；式XV化合物再与式VII所示化合物制备得式XXIII所示化合物后经脱去氨基上的R1得式I所示阿利克伦；本方法具有原料成本低、合成方法简便、易于工业化等优点。
摘要（英）：

The invention relates to a method for preparing aliskiren and an intermediate thereof, which belongs to the technical field of the drug preparation method. The method comprises the following steps: obtaining a compound as shown in Formula XXII and a compound as shown in Formula XIX through reaction of 4-bromine-1-methoxy-2-(3-methoxy-propoxy) benzene with isopropyl magnesium chloride and butyllithium, preparing a compound as shown in Formula XXI though reaction with anhydrous lithium bromide after acidylation with methanesulfonic acid, and preparing an aliskiren intermediate in the ether solvent in the action of a Fe-containing catalyst; and preparing the aliskiren as shown in Formula I through removing R1 on amino of a compound as shown in Formula XXIII obtained through reaction of the compound as shown in Formula XV and a compound as shown in Formula VII. The invention has the advantages of low cost of raw materials, simple synthetic method and easy industrialization and the like.

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