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CAS号626-55-1 3-溴吡啶 | CAS号7397-46-8 二乙基甲氧基硼烷 | CAS号1120-87-2 4-溴吡啶 | CAS号106047-28-3 6-溴-2,3'-联吡啶 | CAS号4385-75-5 4-吡啶-3-基苯甲酸 | CAS号4373-67-5 3-(3-甲氧基苯基)吡啶 | CAS号189090-41-3 2-(8-pyridin-3-... | CAS号82261-42-5 4-(吡啶-3-基)苯胺 | CAS号774-53-8 5-溴-2,3-联吡啶 | CAS号581-46-4 3,3'-联吡啶 | CAS号581-50-0 2,3'-联吡啶 | CAS号15862-22-3 3-(5-溴-3-吡啶)吡啶 | CAS号159725-99-2 1-苯基-7- (3-吡啶)-...合成工艺路线路线简述
- 合成目标产物 Diethyl(3-Pyridyl)Borane 主要起始原料 3-Pyridyl Bromide And Methoxydiethylborane
- 7397-46-8 + 626-55-1 = 89878-14-8
反应条件:1.1 Reagents: Ethylmagnesium Chloride Solvents: Tetrahydrofuran
标题:A Practical Synthesis Of Pyridylboranes Via Magnesium-Halogen Exchange
作者:Cai,Weiling; Ripin,David H. Brown
参考文献:Synlett 日期:2002 卷标:(2) 页码:273-274]
7397-46-8 + 626-55-1 = 89878-14-8
反应条件:1.1 Reagents: Butyllithium Solvents: Hexane,Tert-Butyl Methyl Ether; Rt -> -28 °C; -28 °C -> -44 °C1.2 Solvents: Hexane; < -40 °C; 8 H,< -32 °C1.3 Reagents: Acetic Acid Solvents: Methanol,Water; 0.5 H; 2 H,11 - 15 °C
标题:The Synthesis Of Osu 6162: Efficient,Large-Scale Implementation Of A Suzuki Coupling
作者:Lipton,Michael F.; Mauragis,Michael A.; Maloney,Mark T.; Veley,Michael F.; Vanderbor,Dale W.; Et Al
参考文献:Organic Process Research & Development 日期:2003 卷标:7(3) 页码:385-392]
7397-46-8 + 626-55-1 = 89878-14-8
反应条件:1.1 Catalysts: Chloro(1-Methylethyl)Magnesium Solvents: Tetrahydrofuran; 0.5 H,0 - 5 °C1.2 10 - 20 °C; 20 °C -> 5 °C; 6 H,0 - 5 °C1.3 Reagents: Hydrochloric Acid Solvents: Water
标题:Synthesis Of Diethyl(3-Pyridyl)Borane
作者:Zhang,Jing; Jin,Feng-Min
参考文献:Huaxue Gongye Yu Gongcheng (Tianjin 日期:2013 卷标:30(3) 页码:24-27
3-溴吡啶 反应生成 二乙基(3-吡啶基)-硼烷
参考文献:Org. Process Res. Dev. 2003,7,385-392
标题:Org. Process Res. Dev. 2003,7,385-392
专利信息
专利号:EP-0721461-B1
优先权日:1993-09-30
标 题 :Synthesis of 17-(3-pyridyl) steroids
发明人:POTTER GERARD ANDREW; HARDCASTLE IAN ROBERT
权利人:BTG INT LTD
摘要:A method of preparing a 3 beta -hydroxy- or 3 beta -(lower acyloxy) 16,17-ene-17-(3-pyridyl)-substituted steroid, wherein the 3 beta -(lower acyloxy) group of the steroid has from 2 to 4 carbon atoms, which comprises subjecting a 3 beta -hydroxy-16,17-ene-17-iodo or -bromo steroid to a palladium complex-catalysed cross-coupling reaction with a (3-pyridyl)-substituted borane in which the pyridine ring is substituted at the 5-position by an alkyl group of 1 to 4 carbon atoms or is unsubstituted thereat, in a proportion of at least 1.0 equivalent of borane per equivalent of steroid, in an organic liquid which is a solvent for the 3 beta -hydroxy steroidal reaction product, and optionally esterifying the resulting 3 beta -hydroxy steroidal reaction product with an esterifying agent effective to replace the hydroxy group by a said lower acyloxy group, which method comprises (a) carrying out the reaction with not more than 1.2 equivalents of borane per equivalent of steroid or (b) crystallising the product of the cross-coupling reaction from a mixture of acetonitrile and methanol.
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-6403776-B1
优先权日:2000-07-05
标题 :Synthesis of carbamate ketolide antibiotics
发明人:RIPIN DAVID H B; VANDERPLAS BRIAN C; KANEKO TAKUSHI; MCMILLEN WILLIAM T; MCLAUGHLIN ROBERT W
权利人:PFIZER
摘要:The invention relates to a method of preparing a macrolide antibiotic of the formula n wherein R 1 , R 2 , R 3 , R 4 , R 5 are defined above. These antibiotics are useful as antibacterial and antiprotozoal agents in mammals, including man, as well as in fish and birds. The invention also includes novel compounds made by the preparation of the macrolide antibiotic.
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.