CAS: 2446-23-3; (8R,9S,10R,13S,14S,17S)-4-Chloro-17-Hydroxy-10,13,17-Trimethyl-7,8,9,11,12,14,15,16-Octahydro-6H-Cyclopenta[a]Phenanthren-3-One

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CAS号5785-58-0 4-Chloro-17α-me...

4-氯甲睾酮置于2,3-二氯-5,6-二氰基-1,4-苯醌体系中,用 1,4-二氧六环 用作溶剂,化学反应 48.0H,以53%的收率获得4-氯去氢甲基睾酮
参考文献:Metabolism Of Anabolic Steroids In Humans: Synthesis Of 6β-Hydroxy Metabolites Of 4-Chloro-1,2-Dehydro-17α-Methyltestosterone,Fluoxymesterone,And Metandienone
标题:Metabolism Of Anabolic Steroids In Humans: Synthesis Of 6β-Hydroxy Metabolites Of 4-Chloro-1,2-Dehydro-17α-Methyltestosterone,Fluoxymesterone,And Metandienone
摘要:Hydroxylation At Position 6 Beta Of Testosterone I (17 Beta-Hydroxyandrost-4-En-3-One) And The Anabolic Steroids 17 Alpha-Methyltestosterone Ii (17 Beta-Hydroxy-17 Alpha-Methylandrost-4-En-3-One),Metandienone Iii (17 Beta-Hydroxy-17 Alpha-Methylandrosta-1,,4-Dien-3-One),4-Chloro-1,2-Dehydro-17 Alpha-Methyltestosterone Iv (4-Chloro-17 Beta-Hydroxy-17 Alpha-Methylandrosta-1,4-Dien-3-One),And Fluoxymesterone V (9-Fluoro-11 Beta,17 Beta-Dihydroxy-17 Alpha-Methylandrost-4-En-3-One) Was Achieved Via Light-Induced Autooxidation Of The Corresponding Trimethylsilyl 3,5-Dienol Ethers Dissolved In Isopropanol Or Ethanol. The Reaction Further Yielded The 6 Alpha-Hydroxy Isomer In Low Amounts. The 6 Beta-Hydroxy Isomers Of I-V And The 6 Alpha-Hydroxy Isomers Of I,Iii,And Iv Were Isolated And Characterized By H-1 And C-13 NMR,High-Performance Liquid Chromatography,Gas Chromatography,And Mass Spectrometry. Human Excretion Studies With Single Administered Doses Of Boldenone (17 Beta-Hydroxyandrosta-1,4-Dien-3-One),4-Chloro-1,2-Dehydro-17 Alpha-Methyltestosterone,Fluoxymesterone,Metandienone,17 Alpha-Methyltestosterone,And [16,16,17-H-2(3)]Testosterone Showed That 6 Beta-Hydroxylation Is The Major Metabolic Pathway In The Metabolism Of 4-Chloro-1,2-Dehydro-17 Alpha-Methyltestosterone,Fluoxymesterone,And Metandienone,Whereas For Boldenone,17 Alpha-Methyltestosterone,And Testosterone,6 Beta-Hydroxylation Is Negligable.
Doi:10.1016/0039-128X(95)00008-E

专利信息

专利号:US-2025281509-A1
优先权日:2021-04-26
标 题 :Sequential hormone therapy to improve survival and enhance response to immune therapy in men with prostate cancer
发明人：DENMEADE SAMUEL R; ISAACS JOHN T; ANTONARAKIS EMMANUEL S; KACHHAP SUSHANT; MARKOWSKI MARK CHRISTOPHER
权利人:UNIV JOHNS HOPKINS
摘要:Disclosed are methods for treating men with castrate resistant prostate cancer with a sufficient dose of testosterone to achieve supraphysiologic serum levels of testosterone in sequence with androgen ablative treatment or androgen synthesis inhibitors for one or more cycles until evidence of radiographic progression, at which point the subject will receive immune checkpoint blockade therapy.