A chemoenzymatic synthesis of an androgen receptor antagonist

Vaidyanathan R; Hesmondhalgh L; Hu SH

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A chemoenzymatic synthesis of an androgen receptor antagonist

机译：化学酶法合成雄激素受体拮抗剂

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A new scalable enzymatic resolution approach to both enantiomers of trans-2-hydroxycyclohexanecarbonitrile (9 and 11) was developed. Treatment of the racemic mixture (4) with succinic anhydride in the presence of Novozym 435 led to selective acylation of one enantiomer to the corresponding hemisuccinate, which was separated from the unreacted enantiomer by a simple basic extraction. This procedure produced the desired enantiomer in high ee, while obviating the need for chromatography or expensive catalysts and ligands. The application of this protocol to the large-scale synthesis of an androgen receptor antagonist (1) is described.

机译：对反式-2-羟基环己烷甲腈（9和11）的两个对映异构体开发了一种新的可扩展的酶促拆分方法。在Novozym 435存在下，用琥珀酸酐处理外消旋混合物（4）导致一种对映异构体选择性酰化为相应的半琥珀酸酯，通过简单的碱性萃取将其与未反应的对映异构体分离。该方法以高ee产生所需的对映异构体，同时消除了对色谱法或昂贵的催化剂和配体的需求。描述了该方案在雄激素受体拮抗剂（1）的大规模合成中的应用。

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《Organic process research & development》 |2007年第5期|共4页
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Vaidyanathan R; Hesmondhalgh L; Hu SH;
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1. A chemoenzymatic synthesis of an androgen receptor antagonist [J] . Vaidyanathan R, Hesmondhalgh L, Hu SH Organic process research & development . 2007,第5期

机译：化学酶法合成雄激素受体拮抗剂
2. Androgen action on hepatic vitellogenin synthesis in the eel, Anguilla japonica is suppressed by an androgen receptor antagonist. [J] . Kwon HC, Choi SH, Kim YU, The Journal of Steroid Biochemistry and Molecular Biology . 2005,第2期

机译：雄激素受体拮抗剂可抑制雄鳗对鳗鱼肝脏卵黄蛋白原合成的作用。
3. A chemoenzymatic approach to the synthesis of the stereoisomers of a beta-adrenergic receptor antagonist [J] . Dallanoce C., Carrea G., Secundo F., Tetrahedron, Asymmetry: The International Journal for Repid Publication on all Aspects of Asymmetry in Orgainc, Inorganic, Organometallic, Physical and Bio-Organic Chemistry . 2000,第13期

机译：化学酶法合成β-肾上腺素能受体拮抗剂的立体异构体
4. IN SILICO AND IN VITRO STUDIES OF BENZOHYDRAZIDE ANALOGUES AS POTENT ANDROGEN RECEPTOR ANTAGONIST [C] . H.A.Arjun, Ravi Kumar Rajan, R.Elancheran Conference on Drug Design and Discovery Technologies . 2020

机译：在苯肼类似物的硅和体外研究中作为有效的雄激素受体拮抗剂
5. Design, synthesis and docking models of estrogen and androgen receptor antagonists. [D] . Tinder, Robert J. 2010

机译：雌激素和雄激素受体拮抗剂的设计，合成和对接模型。
6. Design synthesis and biological evaluation of novel androst-17β-amide structurally related compounds as dual 5α-reductase inhibitors and androgen receptor antagonists [O] . Kejing Lao, Guoliang Xun, Xingchun Gou, 2019

机译：设计合成和生物学评估新型的与rost-17β-酰胺结构相关的化合物作为双重5α-还原酶抑制剂和雄激素受体拮抗剂
7. The Androgen Receptor Recruits Nuclear Receptor CoRepressor (N-CoR) in the Presence of Mifepristone via Its N and C Termini Revealing a Novel Molecular Mechanism for Androgen Receptor Antagonists [O] . Myles C. Hodgson, Inna Astapova, Shinta Cheng, 2005

机译：雄激素受体通过其N和C Termini揭示雄激素受体拮抗剂的新分子机制，促进核受体核心压制体（N-COR）。揭示一种新的雄激素受体拮抗剂的新分子机制

A chemoenzymatic synthesis of an androgen receptor antagonist

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