Nordmann R, Petcher T J
J Med Chem. 1985 Mar;28(3):367-75. doi: 10.1021/jm00381a017.
A synthesis of all four diastereoisomeric 3-(tert-butoxycarbonyl)-1,6-dimethoxyoctahydrobenzo[g]quinolines 13a-d is presented. The two trans isomers 13b and 13c have been converted to tricyclic analogues 20 (CV 205-502) and 26 (205-503) of the potent dopaminomimetic ergolines CQ 32-084 and pergolide, respectively. These two compounds combine the essential moiety of apomorphine with the important 8-substituents of ergolines. Preliminary pharmacological evaluation of 20 and 26 suggests that these novel dopamine agonists combine the specificity of apomorphine with the potency, long duration of action, and good oral activity of the ergolines.
本文介绍了所有四种非对映异构的3-(叔丁氧羰基)-1,6-二甲氧基八氢苯并[g]喹啉13a - d的合成。两种反式异构体13b和13c已分别转化为强效拟多巴胺麦角灵CQ 32 - 084和培高利特的三环类似物20（CV 205 - 502）和26（205 - 503）。这两种化合物将阿扑吗啡的基本部分与麦角灵重要的8-取代基结合在一起。对20和26的初步药理学评估表明，这些新型多巴胺激动剂结合了阿扑吗啡的特异性以及麦角灵的效力、长效作用和良好的口服活性。
