专利号:WO-9419366-A1 优先权日:1993-02-26 标题 :Chemical synthesis of squalamine 发明人:MORIARTY ROBERT M; GUO LIANG; TULADHAR SUDERSAN M 权利人:MAGAININ PHARMA 摘要:Methods for the chemical preparation or synthesis of the sterol antibiotic squalamine. Preferably, the preparation is by modifying the 3-position of a 3-oxo-7α-hydroxy-24z-ether protected alcohol group-5α-cholestane with a spermidino moiety to form a 3β-spermidino-7α-hydroxy-24z-ether protected group -5α-cholestane; deprotecting the 24-position of the 3β-spermidino-7α-hydroxy-24z-ether protected group-5α-cholestane to the free hydroxyl; and sulfating the 24-position of the 3β-spermidino-7α, 24-dihydroxy-5α-cholestane.
专利号:US-3595883-A 优先权日:1969-06-16 标 题 :Process for the preparation of 14beta-hydroxy - 17 -keto - 15 - androstenes and novel intermediates produced thereby 发明人:AFONSO ADRIANO 权利人:SCHERING CORP 摘要:14B-HYDROPEROXY-15-ANDROSTEN-17-ONES, PREPARED BY THE ACTION OF OXYGEN ON 14-ANDROSTEN-17-ONES, UPON TREATMENT WITH A MILD REDUCING AGENT YEILDS 14B-HYDROXY-15ANDROSTEN-17-ONES, USEFUL INTERMEDIATES IN THE SYNTHESIS OF STERODIAL CARDENOLIDES. PREFERRED SPECIES ARE 14 B-HYDROPEROXY-5A-15 ANDROSTEN3B-OL-17-ONE 3-ACETATE AND THE 5B-EPIMER THEREOF (PREPARED BY THE ACTION OF OXYGEN OR 5A-14-ANDROSTEN-3B-OL17-ONE 3-ACETATE AND THE 5B-EPIMER THEREOF, RESPECTIVELY) EACH OF WHICH, UPON MILD REDUCTION, PREFERABLY WITH TRIETHYL PHOSPHITE, YEILDS 14B-HYDROXY-5A-15-ANDROSTEN-3BOL-17-ONE 3-ACETATE AND THE 5B-EPIMER THEROF, RESPECTIVELY, WHICH ARE USEFUL INTERMEDIATES IN THE SYNTHESIS OF UZARIGENIN AND DIGITOXIGENIN, RESPECTIVELY.
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-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.
1: Purushottamachar P, Thomas E, Thankan RS, Rudchenko V, Huang G, Njar VCO. Large-scale synthesis of galeterone and lead next generation galeterone analog VNPP433-3β. Steroids. 2022 Sep;185:109062. doi: 10.1016/j.steroids.2022.109062. Epub 2022 Jun 8. 641:631-642. doi: 10.1016/j.jcis.2023.03.077. Epub 2023 Mar 15. 14(3):373. doi: 10.3390/biom14030373. 4: Dovbnya DV, Egorova OV, Donova MV. Microbial side-chain degradation of ergosterol and its 3-substituted derivatives: a new route for obtaining of deltanoids. Steroids. 2010 Oct;75(10):653-8. doi: 10.1016/j.steroids.2010.04.001. Epub 2010 Apr 10. 280(1):C53-60. doi: 10.1152/ajpcell.2001.280.1.C53. 140(3):487-99. doi: 10.1038/sj.bjp.0705460. Epub 2003 Aug 26.
合成参考文献
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