- 英文名称(2R,3R,3As,7R,8As,9S,10Ar,11S,12R,13Ar,13Bs,15S,18S,21S,24S,26R,28R,29As)-2-[(2S)-3-Amino-2-Hydroxypropyl]Hexacosahydro-3-Methoxy-26-Methyl-20,27-Bis(Methylene)-11,15:18,21:24,28-Triepoxy-7,9-Ethano-12,15-Methano-9H,15H-Furo[3,2-I]Furo[2',3':5,6]Pyrano[4,
- 中文名称艾日布林
- IUPAC名称(2S,5S,8S,11S,13R,15R,16aS,18R,19R,19aS,23R,24aS,25S,26aR,27S,28R,29aR,29bS)-18-((S)-3-amino-2-hydroxypropyl)-19-methoxy-13-methyl-7,14-dimethylenehexacosahydro-25H-2,27:5,8:11,15-triepoxy-23,25-ethano-2,28-methanofuro[3,2-i]furo[2',3':5,6]pyrano[4,3-b][1,4]dioxacyclopentacosin-21(3H)-one
- CAS编号253128-41-5
- MFCD编号:MFCD23160037
- EINECS号:803-583-7
- FDA UNII编号:LR24G6354G
- 分子式:C40H59NO11
- 分子量:729.9
- 产品CID: 1212574
- 同类组份化合物CAS253128-41-5 (free base)441045-17-6 (mesylate)
- 产品分类有机原料→分子砌块→桥环类化合物→其它桥环类化合物
相似化合物
253128-67-5欧盟法规
C&L通报上下游产品
艾瑞布林中间体 (1S,3S,6S,9S,12S,14R,16R,18S,20R,21R,22S,26R,29S,31R,32S,33R,35R,36S)-20-[(2S)-2,3-Dihydroxypropyl]-21-Methoxy-14-Methyl-8,15-Bis(Methylene)-2,19,30,34,37,39,40,41-Octaoxanonacyclo[24.9.2.13,32.13,33.16,9.112,16.018,22.029,36.031,35]Hentetracontan-24-One 253128-15-3
[(2S)-2-Hydroxy-3-[(1S,3S,6S,9S,12S,14R,16R,18S,20R,21R,22S,26R,29S,31R,32S,33R,35R,36S)-21-Methoxy-14-Methyl-8,15-Dimethylidene-24-Oxo-2,19,30,34,37,39,40,41-Octaoxanonacyclo[24.9.2.13,32.13,33.16,9.112,16.018,22.029,36.031,35]Hentetracontan-20-Yl]Propyl] Methanesulfonate 253128-19-7合成工艺路线路线简述
- 合成目标产物 Eribulin 主要起始原料 5-(N,N-Dibenzylglycyl)Salicylamide
- (文献来源)合成步骤主要原料 5-(N,N-Dibenzylglycyl)Salicylamide
(1S,3S,6S,9S,12S,14R,16R,18S,20R,21R,22S,26R,29S,31R,32S,33R,35R,36S)-20-[(2S)-3-Azido-2-Hydroxypropyl]-21-Methoxy-14-Methyl-8,15-Bis(Methylidene)-2,19,30,34,37,39,40,41-octaoxanonacyclo[24.9.2.13,32.13,33.16,9.112,16.018,22.029,36.031,35]Hentetracontan-24-One置于水,三甲基膦体系中,用 四氢呋喃 用作溶剂,化学反应 22.0H,以87%的收率获得艾瑞布林
参考文献:Methods Useful In The Synthesis Of Halichondrin B Analogs
标题:Methods Useful In The Synthesis Of Halichondrin B Analogs
摘要:总的来说,本发明涉及改进的方法,用于合成半龙脂素b的类似物,如厄立宾及其药用盐(例如,厄立宾甲磺酸盐).
专利信息
专利号:US-11873305-B2
优先权日:2020-06-30
标题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds
发明人:ZHANG HAIMING; XU JIE; WUITSCHIK GEORG; ANGELAUD REMY; HEROLD SEBASTIAN; STUTZ ALFRED; BRUETSCH TOBIAS; BURKHARD JOHANNES
权利人:GENENTECH INC; HOFFMANN LA ROCHE
摘要:Provided herein are processes for the preparation of indolyl intermediates using Wenker Synthesis for the total synthesis of SERD compounds useful in the treatment of cancer.
专利号:US-11542269-B2
优先权日:2018-01-03
标 题:Prins reaction and compounds useful in the synthesis of halichondrin macrolides and analogs thereof
发明人:CHOI HYEONG-WOOK; FANG FRANCIS G
权利人:EISAI R&D MAN CO LTD
摘要:The invention provides methods utilizing Prins reaction in the preparation of compounds that may be useful as intermediates in the synthesis of halichondrin macrolides and analogs thereof. The invention also provides compounds that may be useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.
专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as
专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.
专利号:US-9695188-B2
优先权日:2013-12-06
标 题 :Methods useful in the synthesis of halichondrin B analogs
发明人:HU YONGBO; ZHANG HUIMING; CHIBA HIROYUKI; KOMATSU YUKI; LEWIS BRYAN M
权利人:EISAI R&D MAN CO LTD
摘要:In general, the present invention features improved methods useful for the synthesis of analogs of halichondrin B, such as eribulin and pharmaceutically acceptable salts thereof (e.g., eribulin mesylate).
专利号:US-11713329-B2
优先权日:2018-12-10
标 题 :Intermediates useful in the preparation of halichondrin compounds and methods for preparing the same
发明人:XU WEIPING
权利人:BEIJING TIENYI LUFU PHARMATECH CO LTD
摘要:The invention relates to intermediates useful in the preparation of halichondrin compounds, methods for preparing the same and use thereof, such as halichondrins, eribulin, or their analogs. The intermediates, the methods and use thereof are used for the synthesis of the C20-C26 fragment of halichondrin compounds. The raw materials in the synthetic route of the invention are cheap and easily obtained, the sources and the qualities of the raw materials are reliable. The choice of the methods useful in the synthesis of chiral central structures are based on the structural characteristics of the reactants, thus effectively improving the synthesis efficiency, reducing the difficulties and risks of product quality control, and avoiding the use of highly toxic and expensive organotin catalysts to significantly decrease costs and improve environmental friendliness.