一些芳香族前列腺素类似物的合成。
Synthesis of some aromatic prostaglandin analogs.
作者信息
Perchonock C D, Loev B
出版信息
Prostaglandins. 1978 Apr;15(4):623-7. doi: 10.1016/0090-6980(78)90057-6.
PMID:674693
Abstract
Some aromatic prostaglandin analogs, having a benzene (2a, 2b) and a dimethoxybenzene (1) ring in place of the cyclopentane moiety, have been synthesized. The key intermediates in the syntheses were lactols 9 and 5, which were elaborated to the final products via two olefination reactions. Compound 2b was twice as potent as phenylbutazone and nine times as potent as aspirin in inhibiting prostaglandin synthetase activity.
摘要
已经合成了一些芳香族前列腺素类似物，它们用苯环（2a，2b）和二甲氧基苯环（1）取代了环戊烷部分。合成中的关键中间体是内酯9和5，它们通过两步烯化反应被转化为最终产物。在抑制前列腺素合成酶活性方面，化合物2b的效力是保泰松的两倍，是阿司匹林的九倍。
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