CAS: 1257044-40-8; 2-((1H-Pyrrolo[2,3-B]Pyridin-5-yl)Oxy)-4-(4-((4'-Chloro-5,5-Dimethyl-3,4,5,6-Tetrahydro-[1,1'-Biphenyl]-2-yl)Methyl)Piperazin-1-yl)-N-((3-Nitro-4-(((Tetrahydro-2H-Pyran-4-yl)Methyl)Amino)Phenyl)Sulfonyl)Benzamide

上下游产品

3-nitro-4-(((tetrahydro-2H-pyran-4-yl)methyl)amino)benzenesulfonamide [2-((1H-pyrrolo [2,3-b]pyridin-5-yl)oxy)-4-(4-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid] 4-tetrahydropyranmethylamine 4-fluoro-3-nitrobenzenesulfonamide 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide sulfate

在 Lithium Hydroxide体系中,用 甲醇 用作溶剂,以90%的收率获得维特克拉
参考文献:一种bcl-2抑制剂-维特克拉的制备方法
标题:一种bcl-2抑制剂-维特克拉的制备方法
摘要:本发明公开一种bcl‑2抑制剂‑维特克拉的制备方法,主要包括六个步骤,1)以vm1和vm2为反应起始原料,在碱催化作用下对接反应,制备得到中间体v1;2)中间体v1在碱催化作用下,与boc哌嗪反应制备得到中间体v2;3)中间体v2在酸试剂作用下,脱去boc保护,制备得到中间体v3;4)中间体v3和vm3经加热反应形成席夫碱,再在还原剂作用下,将席夫碱转变为仲胺,制备得到中间体v4;5)中间体v4与vm4在缩合剂作用下反应制备得到酰胺化合物中间体v5;6)中间体v5在催化剂催化下,脱去苯磺酰基保护基,得到终产品venetoclax.相对于现有技术路线,该工艺路线步骤简短,反应简便易行,适合于大规模工业化生产.

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-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-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人：MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

专利号:EP-4421075-A1
优先权日:2023-02-27
标 题 :Process for the preparation of venetoclax and intermediates used therein
发明人：BERGANT SIMONCIC ANA
权利人:KRKA D D NOVO MESTO
摘要:The invention relates to a process for the synthesis of Venetoclax. The invention further relates to intermediates that are useful in the synthesis of Venetoclax.

专利号:EP-3412666-A1
优先权日:2017-06-07
标 题:Process and intermediates for the preparation of bcl-2 inhibitors including venetoclax through reductive amination
发明人：GREGG BRIAN THOMAS; GEISS WILLIAM BERT; HERR ROBERT JASON
权利人:ALBANY MOLECULAR RES INC
摘要:The invention relates to a process for the preparation of compounds of formula (I), which are useful intermediates in the synthesis of Venetoclax and structurally related compounds, by reductive amination of a compound of formula (II).