CAS: 154229-18-2; Abiraterone Acetate

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CAS号115375-60-5 (3BETA)-雄甾-5,16... | CAS号1692-25-7 吡啶-3-硼酸 | CAS号108-24-7 乙酸酐 | CAS号154229-19-3 阿比特龙 | CAS号75-36-5 乙酰氯 | CAS号626-55-1 3-溴吡啶 | CAS号89359-48-8 [10,13-dimethyl... | CAS号853-23-6 醋酸去氢表雄酮 | CAS号89878-14-8 二乙基(3-吡啶基)硼烷 | CAS号53-43-0 去氢表雄酮 | CAS号154229-19-3 阿比特龙

在 盐酸羟胺体系中,用 乙腈 用作溶剂,以97%的收率获得乙酸阿比特龙酯
参考文献:一种合成醋酸阿比特龙新方法
标题:一种合成醋酸阿比特龙新方法
摘要:本发明涉及一种合成醋酸阿比特龙新方法,属于药物合成领域,更具体地说,涉及治疗晚期前列腺癌药物醋酸阿比特龙新的合成方法以及合成方法中涉及到的新的中间体化合物的制备方法.本发明采用醋酸妊娠双烯醇酮为原料,经甲基r基亚砜锂试剂的加成和重排反应得到丙烯醇产物3,丙烯醇3经氧化及杂d‑a,异构化,乙酰化等反应合成目标化合物醋酸阿比特龙.本发明解决了现有技术存在的合成原料较贵的成本问题,提供了一种收率高,环境污染小,纯化简便的制备阿比特龙和醋酸阿比特龙的方法,此法比较易于放大到工业化生产.

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-2022118094-A1
优先权日:2019-02-21
标题:Synthesis of biomimetic cell wall structure
发明人：WANG YONG; SHI PENG
权利人:PENN STATE RES FOUND
摘要:The present invention relates generally to methods of generating a biomimetic cell wall (BCW) on a target surface, compositions comprising the BCW, and methods of use of the compositions, including biomedical applications of the BCW coated compositions.

专利号:WO-2013030410-A3
优先权日:2011-12-23
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 processesfor obtaining abirateroneand 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.