CAS: 53-43-0; Dehydroepiandrosterone

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雄烯二醇置于4-二甲氨基吡啶,四丁基氟化铵,三乙胺体系中,用 二氯甲烷 作为反应溶剂,化学反应生成 去氢表雄酮
参考文献:用于醇选择性氧化的氟铬酸吡啶鎓或氯铬酸苄基三甲基铵
标题:用于醇选择性氧化的氟铬酸吡啶鎓或氯铬酸苄基三甲基铵
摘要:在伯醇存在下仲醇的选择性氧化已通过以下顺序实现,(1) 用 T-Bume2Sicl 选择性保护伯醇,(2) 用标题试剂氧化仲醇,以及 (3) 伯醇的脱保护羟基.
DOI:10.1246/bcsj.57.2019

专利信息

专利号:US-9884067-B2
优先权日:2013-03-14
标 题:Androgen receptor down-regulating agents and uses thereof
发明人：NJAR VINCENT C O; GEDIYA LALJI K; PURUSHOTTAMACHAR PURANIK; GODBOLE ABHIJIT; KWEGYIR AFFUL ANDREW; VASAITIS TADAS
权利人:UNIV OF MARYLAND EASTERN SHORE; UNIV JEFFERSON; UNIV MARYLAND
摘要:The present disclosure provides the design and synthesis of novel steroidal compounds that cause down-regulation of the androgen receptor (AR), both full length and splice variant. The compounds are potential agents for the treatment of all forms of prostate cancer and other diseases that depend on functional AR.

专利号:US-2014011992-A1
优先权日:2012-12-20
标 题:Synthesis of abiraterone and related compounds
发明人：PEREZ ENCABO ALFONSO; TURIEL HERNANDEZ JOSE ANGEL; GALLO NIETO FRANCISCO JAVIER; LORENTE BONDE-LARSEN ANTONIO; SANDOVAL RODRIGUEZ CELSO MIGUEL
权利人:CRYSTAL PHARMA SAU
摘要:The present invention relates to processes for obtaining abiraterone and derivatives thereof, such as abiraterone acetate, by means of a Suzuki coupling through a steroid borate of general formula (IV) or a C—C coupling through a steroid hydrazone of general formula (II), as well as to intermediates useful in said processes.

专利号:US-9650410-B2
优先权日:2013-07-29
标题:Process for the preparation of abiraterone and abiraterone acetate
发明人：LENNA ROBERTO; DI BRISCO RICCARDO
权利人:IND CHIMICA SRL
摘要:The present invention relates to a novel process for the synthesis of abiraterone, and in particular of abiraterone acetate, compound of formula (I) reported below: N O (I) which has pharmacological activity useful for slowing down the progression of prostate cancer at an advanced stage. The process is characterized by an intermediate step wherein DHEA-acetate is triflated using Ar—N(OTf) 2 as the triflation reagent.

专利号:US-8975244-B2
优先权日:2012-07-25
标题:Process and intermediates for the preparation of abiraterone acetate
发明人：MAROM EHUD; RUBNOV SHAI; MIZHIRITSKII MICHAEL
权利人:MAPI PHARMA LTD
摘要:The present invention relates to a process for the synthesis of (3beta)17-(3-pyridinyl)androsta-5,16-dien-3-yl acetate (Abiraterone acetate) represented by the structure of formula (1), and salts thereof, especially salts with pharmaceutically acceptable acids. The present invention further relates to certain intermediates in such processes.

专利号:US-9676815-B2
优先权日:2013-07-29
标题:Process for the preparation of abiraterone or abiraterone acetate
发明人：LENNA ROBERTO; DI BRISCO RICCARDO
权利人:IND CHIMICA SRL
摘要:The present invention relates to a novel process for the synthesis of abiraterone and in particular abiraterone acetate, a compound of formula (I) reported below: having pharmacological activity suitable for slowing down the progression of advanced stage prostate cancer. The process is characterized by the fact that the intermediate triflation step is carried out on prasterone (DHEA) or its 3-acetate using Ar—N(OTf) 2 as the triflation reagent, but where Ar is not phenyl, and by the fact that the base used in this step is an alkali metal alcoholate.

专利号:US-9295679-B2
优先权日:2008-03-25
标 题:Prodrugs of C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity
发明人：NJAR VINCENT; BRODIE ANGELA; GEDIYA LALJI K
权利人:UNIV MARYLAND
摘要:Prodrugs of steroidal C-17 benzoazoles, pyrimidinoazoles (az-abenzoazoles) and diazines. Methods of synthesis are also described, whereby a prodrug group is substituted for a functional group at A ring portion of the ABC ring structure of the steroid. Suitable pro-drug groups include amino acid groups, succinate groups, phosphate groups, or sulfamate groups. The prodrugs of the disclosed compounds allow for improved oral bioavailability of the compounds that are inhibitors of human CYP 17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds and the corresponding prodrugs are useful for the treatment of conditions such as human prostate cancer, breast cancer, and prostate hyperplasia.