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[螺内酯、坎利酮及2-甲基-坎利酮的乙酰化反应]

[Acetylation of spironolactone, canrenone and 2-methyl-canrenone].

作者信息

Görlitzer K, Moormann P, Pollow K, Schaffrath M

机构信息

Institut für Pharmazeutische Chemie, Technischen Universität Braunschweig.

出版信息

Arch Pharm (Weinheim). 1995 Feb;328(2):161-3. doi: 10.1002/ardp.19953280213.

DOI:10.1002/ardp.19953280213
PMID:7726743
Abstract

Reaction of the title compounds with acetic anhydride and acetyl chloride yields the 3,5-dien-3-yl acetate 2, the isomeric 2,4,6- and 3,5,7-trien-3-yl acetates 3 and 4 as well as the 2,4,6,8(14)-tetraen-3-yl acetate 7. The 2 alpha-methyl-8,14-didehydro-canrenone (9) is obtained by hydrolysis of 7. Binding affinities of 7 and 9 to hormone receptors as well as serum proteins (SHBG, CBG) are investigated. The compounds are inactive.

摘要

标题化合物与乙酸酐和乙酰氯反应生成3,5 - 二烯 - 3 - 基乙酸酯2、异构体2,4,6 - 和3,5,7 - 三烯 - 3 - 基乙酸酯3和4以及2,4,6,8(14) - 四烯 - 3 - 基乙酸酯7。通过7的水解得到2α - 甲基 - 8,14 - 二脱氢坎利酮(9)。研究了7和9与激素受体以及血清蛋白(性激素结合球蛋白、皮质类固醇结合球蛋白)的结合亲和力。这些化合物无活性。

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