申请人:Societe de Conseils de Recherches et d'Applications Scientifiques
公开号:US04581363A1
公开(公告)日:1986-04-08
This invention relates to 1,3-dihydro-6-methyl-7-hydroxy-furo-(3,4-c)-pyridine derivatives of the general formula I ##STR1## wherein each of A.sub.1 and A.sub.2 independently represents various hydrocarbon groups and therapeutically acceptable addition salts thereof; to a process for the preparation of the same comprising oxidizing the secondary alchol .alpha..sup.4, 3-o-isopropylidene-1-methyl-5-(1-hydroxy-1-A.sub.1)-methyl pyridine by any usual technique, reacting the resultant ketone with a compound of the general formula XA.sub.2 wherein X stands for Br or I in the presence of magnesium in diethyl ether at the boil and treating the resultant tertiary alcohol with an acidic agent to provoke breaking of the isopropylidene ring and 3,4-cyclization; and to pharmaceutical compositions containing these derivatives.
本发明涉及一般式I的1,3-二氢-6-甲基-7-羟基呋喃-(3,4-c)-吡啶衍生物,其中A.sub.1和A.sub.2各自独立地表示各种碳氢基团及其治疗可接受的加合盐;制备该化合物的方法包括通过任何通常的技术将二级醇α.4,3-o-异丙基-1-甲基-5-(1-羟基-1-A.sub.1)-甲基吡啶氧化,将所得的酮与一般式XA.sub.2的化合物在二乙醚中镁沸腾的存在下反应,然后用酸性试剂处理所得的三级醇以引发异丙基亚甲基环的断裂和3,4-环化;以及含有这些衍生物的制药组合物。