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    • 3. 发明申请
    • A METHOD OF REMOVING THE TRIPHENYLMETHANE PROTECTING GROUP
    • 一种去除三苯甲基保护基团的方法
    • WO2005021535A3
    • 2005-06-09
    • PCT/CZ2004000051
    • 2004-08-26
    • ZENTIVA ASRADL STANISLAVSTACH JANKLECAN ONDREJ
    • RADL STANISLAVSTACH JANKLECAN ONDREJ
    • C07D257/04C07D403/10
    • C07D257/04C07D403/10Y02P20/55
    • A method of removing the triphenylmethane protecting group from 1-triphenylmethyl-5-(4'-subst. methyl-1,1'-biphenyl-2-yl)-1H-tetrazoles of general formula I wherein R represents the groups of formulae and where R , R and R can be H, a halogen, an unbranched or branched C1-C5 alkyl, C1-C5 hydroxyalkyl, Cl-C5 alkoxy, C1-C5 alkoxymethyl or benzyl, or wherein R and R can form together a saturated or unsaturated C5-C7 ring, optionally an unsubstituted or substituted aromatic ring, is carried out by solvolysis in a simple anhydrous Cl to C5 alcohol in a neutral or slightly basic medium. The method is suitable for the preparation of drugs, such as the potassium salts of losartan, irbesartan or valsartan or candesartan cilexetil.
    • 从通式I的1-三苯基甲基-5-(4'-取代甲基-1,1'-联苯-2-基)-1H-四唑中除去三苯基甲烷保护基的方法,其中R表示式的基团和 其中R 1,R 2和R 3可以是H,卤素,无支链或支链C 1 -C 5烷基,C 1 -C 5羟烷基,C 1 -C 5烷氧基,C 1 -C 5烷氧基甲基或苄基,或其中 R 2和R 3可以一起形成饱和或不饱和的C 5 -C 7环,任选未取代或取代的芳环,通过在中性或微碱性介质中的简单的无水C1至C5醇中溶剂解来进行。 该方法适用于制备药物,如氯沙坦,厄贝沙坦或缬沙坦或坎地沙坦酯的钾盐。