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    • 13. 发明授权
    • C-Homo-9-oxa-ergolines
    • C-同-9-氧杂 - 麦角碱
    • US4503053A
    • 1985-03-05
    • US532740
    • 1983-09-15
    • Lucien NedelecJean-Claude GascPatrick Fauveau
    • Lucien NedelecJean-Claude GascPatrick Fauveau
    • A61K31/535A61P25/00A61P43/00C07D209/00C07D265/00C07D498/06
    • C07D209/94C07D498/06
    • Novel C-homo-9-oxa-ergolines of the formula ##STR1## wherein R is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, R.sub.1 is selected from the group consisting of hydrogen, chlorine and bromine or taken with b forms .dbd.0, a and b form a carbon-carbon bond or a is hydrogen when R.sub.1 and b form .dbd.0, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms, aralkyl of 7 to 12 carbon atoms and cycloalkylalkyl of 4 to 7 carbon atoms, R.sub.3 is selected from the group consisting of hydroxymethyl, alkylthiomethyl of 1 to 5 alkyl carbon atoms, cyanomethyl, carboxy optionally esterified with an aliphatic alcohol of 1 to 5 carbon atoms and ##STR2## R.sub.4 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, R.sub.5 is alkyl of 1 to 4 carbon atoms or R.sub.4 and R.sub.5 taken with the nitrogen atom form a saturated heterocycle optionally containing a second heteroatom having dopaminergic agonist, serotoninergic and antihypertensive activity as well as prolactin secretion inhibition and antianoxic activities and their preparation and intermediates.
    • 式(Ⅰ)的新型C-高-9-氧杂 - 麦角醇其中R选自氢和1至4个碳原子的烷基,R 1选自氢,氯和溴或 以b形式= 0取代,a和b形成碳 - 碳键,或者当R 1和b形成= 0时,a为氢,R 2选自氢,1至4个碳原子的烷基,7至 12个碳原子和4至7个碳原子的环烷基烷基,R 3选自羟甲基,1至5个烷基碳原子的烷基硫甲基,氰基甲基,任选被1至5个碳原子的脂族醇酯化的羧基, R4选自氢和1-4个碳原子的烷基,R5是1-4个碳原子的烷基或R4和R5与氮原子一起形成饱和杂环,任选地含有具有多巴胺能激动剂的第二个杂原子,5-羟色胺能 和抗高血压活动 以及催乳素分泌抑制和抗氧化活性及其制备和中间体。