钯催化雌酮的交叉偶联反应

IF 2.1 4区医学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY

Steroids Pub Date : 2025-05-06 DOI:10.1016/j.steroids.2025.109627

Peter Langer

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引用次数: 0

摘要

钯催化雌酮的交叉偶联反应允许合成各种替代类固醇，这是不易通过其他方法获得的。产品包括各种炔基化和芳基化雌酮和13α-雌酮，16-芳基甲基-3- o -甲基甾酮和16-炔基甲基-3- o -甲基甾酮。反应通常以优异的化学选择性和区域选择性进行，并表现出广泛的官能团耐受性。在一些情况下，所制备的雌酮衍生物被证明是活性和选择性的碱性磷酸酶抑制剂或表现出相当大的抗增殖活性。

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Palladium-catalyzed cross-coupling reactions of estrone

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Palladium-catalyzed cross-coupling reactions of estrone

Palladium catalyzed cross-coupling reactions of estrone allow for the synthesis of a variety of substituted steroids which are not readily available by other methods. Products include various alkynylated and arylated estrones and 13α-estrones, 16-arylmethylidene-3-O-methylestrones and 16-alkynylmethylidene-3-O-methylestrones. Reactions usually proceed with excellent chemo- and regioselectivity and exhibit a broad functional group tolerance. In several cases, the estrone derivatives prepared proved to be active and selective inhibitors of alkaline phosphatases or exhibited considerable antiproliferative activities.

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来源期刊

Steroids 医学-内分泌学与代谢

CiteScore

5.10

自引率

3.70%

发文量

120

审稿时长

73 days

期刊介绍： STEROIDS is an international research journal devoted to studies on all chemical and biological aspects of steroidal moieties. The journal focuses on both experimental and theoretical studies on the biology, chemistry, biosynthesis, metabolism, molecular biology, physiology and pharmacology of steroids and other molecules that target or regulate steroid receptors. Manuscripts presenting clinical research related to steroids, steroid drug development, comparative endocrinology of steroid hormones, investigations on the mechanism of steroid action and steroid chemistry are all appropriate for submission for peer review. STEROIDS publishes both original research and timely reviews. For details concerning the preparation of manuscripts see Instructions to Authors, which is published in each issue of the journal.