申请人:Radl Stanislav
公开号:US20060287537A1
公开(公告)日:2006-12-21
A method of removing the triphenylmethane protecting group from 1-triphenylmethy1-5-(4′-subst. methyl-1,1′-biphenyl-2-yl)-1H-tetrazoles of general formula I wherein R represents the groups of formulae and where R
1
, R
2
and R
3
can be H, a halogen, an unbranched or branched C1-C5 alkyl, C1-C5 hydroxyalkyl, C1-C5 alkoxy, C1-C5 alkoxymethyl or benzyl, or wherein R
2
and R
3
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 C1 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.
一种从一般式I的1-三苯甲基-5-(4'-取代甲基-1,1'-联苯基)-1H-四唑中去除三苯甲基保护基的方法,其中R代表式的基团,其中R1、R2和R3可以是H、卤素、直链或支链C1-C5烷基、C1-C5羟基烷基、C1-C5烷氧基、C1-C5烷氧甲基或苄基,或其中R2和R3可以共同形成饱和或不饱和的C5-C7环,可选地为未取代或取代的芳香环,通过在中性或稍微碱性介质中的简单无水C1到C5醇中进行溶剂解除。该方法适用于制备药物,例如洛卡新钾、厄贝沙坦钾、缬沙坦钾或坎地沙坦西酯盐。