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    • 2. 发明公开
    • NOVEL PROCESSES FOR THE PREPARATION OF LOSARTAN, AND A BENZYLIMIDAZOL DERIVATIVE AS USEFUL INTERMEDIATE FOR PREPARATION THEREOF
    • 用于制备洛沙坦的新方法和作为其制备的有用的中间体的苯并咪唑衍生物
    • KR20070093656A
    • 2007-09-19
    • KR20060023754
    • 2006-03-14
    • LG LIFE SCIENCES LTD
    • KIM YUN SIKPARK BONG JUN
    • C07D233/68C07D233/66
    • A method for preparing a novel imidazole derivative is provided to obtain the imidazole derivative useful as an important intermediate of a losartan derivative used for selectively synthesizing losartan with high yield. And a novel method for preparing the losartan using the imidazole derivative is provided. A method for preparing a compound represented by the formula(2) comprises the steps of: (a) chloroformylating a compound represented by the formula(4) in the presence of a chlorinating agent and a formylating agent to form a compound represented by the formula(3); and (b) reducing an aldehyde group of the compound of the formula(3) into an alcohol. The method for preparing a compound represented by the formula(1) comprises the steps of: (a) performing a [3+2] ring-addition reaction on the compound of the formula(2) with an azide-containing dieneophile in the presence of an anion activating agent to form a compound represented by the formula(1-1); and (b) treating the compound of the formula(1-1) with potassium hydroxide.
    • 提供一种制备新型咪唑衍生物的方法,以获得可用作用于以高产率选择性合成氯沙坦的氯沙坦衍生物的重要中间体的咪唑衍生物。 并提供了使用咪唑衍生物制备氯沙坦的新方法。 制备由式(2)表示的化合物的方法包括以下步骤:(a)在氯化剂和甲酰化剂的存在下将由式(4)表示的化合物氯甲酰化以形成由式 (3); 和(b)将式(3)化合物的醛基还原成醇。 由式(1)表示的化合物的制备方法包括以下步骤:(a)在含有叠氮化物的亲油性物质的情况下,在式(2)的化合物上进行[3 + 2]环加成反应 的阴离子活化剂以形成由式(1-1)表示的化合物; 和(b)用氢氧化钾处理式(1-1)的化合物。