A general synthetic route from elymoclavine (4a) to a variety of C-17 substituted 8-ergolenes has been established. [The C-17 position is the carbon attached to C-8 of the ergoline (1) skeleton as indicated in structure 2.] This route involves displacement reactions on the allylic chloride (4h) prepared from 4a by reaction with thionyl chloride. Conversion of the naturally occurring tricyclic clavines, chanoclavine I (5a) and isochanoclavine I (5b), to the tetracyclic clavine, agroclavine (4i), has been achieved. The new compounds prepared were tested for prolactin-inhibiting ability and were found to possess activity. One of the compounds prepared, 6-methyl-8-ergolenylacetamide (4k), was very potent, comparing favorably in activity to the best prolactin inhibitors reported to date.

译文

已经建立了从elymoclavine (4a) 到多种C-17取代的8-麦角烯的一般合成路线。[C-17位置是附着在麦角灵 (1) 骨架的C-8上的碳,如结构2所示。]该路线涉及通过与亚硫酰氯反应在4a制备的烯丙基氯 (4h) 上的置换反应。已经实现了将天然存在的三环锁骨蛋白 (chanoclavine I (5a) 和isochanoclavine I (5b)) 转化为四环锁骨蛋白 (agroclavine (4i))。测试了制备的新化合物的催乳素抑制能力,并发现其具有活性。制备的化合物之一,6-甲基-8-麦角烯基乙酰胺 (4k) 非常有效,与迄今为止报道的最佳催乳素抑制剂相比,活性具有优势。

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