前列腺素及其类似物。22. 11-脱氧前列腺素E1和E2的11-取代衍生物的合成。潜在的支气管扩张剂。
Prostaglandins and congeners. 22. Synthesis of 11-substituted derivatives of 11-deoxyprostaglandins E1 and E2. Potential bronchodilators.
作者信息
Floyd M B, Schaub R E, Siuta G J, Skotnicki J S, Grudzinskas C V, Weiss M J, Dessy F, VanHumbeeck L
出版信息
J Med Chem. 1980 Aug;23(8):903-13. doi: 10.1021/jm00182a018.
PMID:7401116
Abstract
The interesting bronchodilator activity of l-11-deoxy-11 alpha-[(2-hydroxyethyl)thio]prostaglandin E2 methyl ester (3a) is described. The preparation of 3a and its analogues by Michael-type additions to various members of the PGA series or by total synthesis using the lithiocuprate conjugate addition process is also described. Structure-activity relationships in this series are discussed.
摘要
描述了l-11-脱氧-11α-[(2-羟乙基)硫代]前列腺素E2甲酯(3a)有趣的支气管扩张活性。还描述了通过对PGA系列的各种成员进行迈克尔型加成或使用锂铜酸盐共轭加成法进行全合成来制备3a及其类似物的方法。讨论了该系列中的构效关系。
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