申请人:Meiji Seika Kaisha, Ltd.
公开号:US04189489A1
公开(公告)日:1980-02-19
5-Alkoxy-picolinic acids and the salts and the esters thereof represented by the formula (I): ##STR1## wherein R represents an alkyl group having 1 to 6 carbon atoms and M represents a hydrogen atom; a calcium atom; a sodium atom; a potassium atom; an aluminum atom; an unsubstituted phenyl group; a phenyl group substituted with one or more of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms or a halogen atom (such as a chlorine, bromine, iodine, etc., atom); a phthalidyl group; an alkoxyalkyl group wherein the alkyl moiety and the alkoxy moiety each has 1 to 4 carbon atoms; or an acyloxyalkyl group having the formula ##STR2## wherein R.sub.2 represents a hydrogen atom or a methyl group and R.sub.3 represents an alkyl group having 1 to 5 carbon atoms (such as a methyl, n-propyl, isobutyl, t-butyl, etc., group), an alkoxy group having 1 to 4 carbon atoms, a phenyl group, a phenyl group substituted with one or more of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms or a halogen atom (such as a chlorine, bromine, iodine, etc., atom) or an aralkyl group wherein the alkyl moiety has 1 to 3 carbon atoms, which are useful as anti-hypertensive agents, a process for preparing 5-alkoxy-picolinic acids and the salts and the esters thereof, and anti-hypertensive compositions containing the 5-alkoxy-picolinic acids and the salts and the esters thereof.
式(I)所表示的5-烷氧基吡啶甲酸及其盐和酯,其中R代表具有1至6个碳原子的烷基,M代表氢原子;钙原子;钠原子;钾原子;铝原子;未取代的苯基;取代有一个或多个具有1至4个碳原子的烷基、1至4个碳原子的烷氧基或卤素原子(如氯、溴、碘等)的苯基;邻苯二甲酰基基团;烷氧基烷基团,其中烷基部分和烷氧基部分各自具有1至4个碳原子;或具有下式的酰氧烷基团:
其中R₂代表氢原子或甲基基团,R₃代表具有1至5个碳原子的烷基(例如甲基、正丙基、异丁基、叔丁基等)、1至4个碳原子的烷氧基、苯基、取代有一个或多个具有1至4个碳原子的烷基、1至4个碳原子的烷氧基或卤素原子(如氯、溴、碘等)的苯基或烷基部分具有1至3个碳原子的芳基烷基团。这些化合物可用作降压药,提供了制备5-烷氧基吡啶甲酸及其盐和酯的方法,以及含有5-烷氧基吡啶甲酸及其盐和酯的降压组合物。