申请人:Roussel Uclaf
公开号:US04221809A1
公开(公告)日:1980-09-09
Novel lactones of the formula ##STR1## wherein the dotted line indicates the optional presence of a second bond, A is a single bond or --CH.sub.2 --CH.sub.2 --, R is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.6 is --OR'.sub.A, R'.sub.A is selected from the group consisting of hydrogen, tetrahydropyranyl, alkyl of 1 to 3 carbon atoms and ##STR2## R".sub.A is selected from the group consisting of alkyl of 1 to 3 carbon atoms optionally substituted with carboxyl and phenyl optionally substituted with a member of the group consisting of carboxyl, free hydroxyl, hydroxyl protected with an acyl of 2 to 4 carbon atoms and hydroxyl protected with an easily hydrolyzable group and R and R.sub.6 together form a keto group, R.sub.7 is --(CH.sub.2)m.sub.A --CH.sub.3, m.sub.A is 3,4,5 or 6 and R.sub.6 and R.sub.7 taken together form .dbd. CH--(CH.sub.2)n.sub. A --CH.sub.3 n.sub.A is 2,3,4 or 5 and the wavy lines indicate that the bonds are in one or the other of the possible configurations and when A is a simple bond, the bond between the cyclopentane ring and the oxygen is in the .alpha.-position having hypotensive activity and novel processes and intermediates for their preparation.
公式为##STR1##的新型内酯,其中虚线表示第二键的可选存在,A是单键或--CH.sub.2 --CH.sub.2 --,R选自氢、1到4个碳原子的烷基和2到4个碳原子的烯基和炔基组成的群,R.sub.6是--OR'.sub.A,R'.sub.A选自氢、四氢吡喃基、1到3个碳原子的烷基和##STR2##,R".sub.A选自1到3个碳原子的烷基,可选择地取代羧基和苯基,可选择地取代羧基、游离羟基、用2到4个碳原子的酰基保护的羟基和用易水解基团保护的羟基和R和R.sub.6一起形成酮基,R.sub.7是--(CH.sub.2)m.sub.A --CH.sub.3,m.sub.A为3,4,5或6,R.sub.6和R.sub.7一起形成.dbd. CH--(CH.sub.2)n.sub. A --CH.sub.3,n.sub.A为2,3,4或5,波浪线表示键处于可能的两种配置之一,当A是简单键时,环戊烷环和氧之间的键处于α-位置,具有降压活性,以及其制备的新型过程和中间体。