4-氯-7-氮杂吲哚置于四丁基氟化铵,仲丁基锂,Sodium Hydride,溶剂黄146,锌体系中,用 四氢呋喃,正己烷,环己烷,乙酸乙酯 作为反应溶剂,化学反应 39.17H,反应生成 5-羟基-7-氮杂吲哚 参考文献:Synthesis Of Functionalized 7-Azaindoles Via Directed Ortho-Metalations 标题:Synthesis Of Functionalized 7-Azaindoles Via Directed Ortho-Metalations 摘要:Functionalization At C-5 Of 4-Fluoro-And 4-Chloro-1-Triisopropylsilyl-7-Azaindole,1 And 2,Respectively,Leads To A Variety Of New Substituted 7-Azaindole Derivatives. We Also Describe Two Approaches To Introduce Functionality At C-6. (C) 2004 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Tetlet.2004.01.122
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).
专利号:US-2022073513-A1 优先权日:2018-12-29 标题:1h-pyrrolo[2,3-b]pyridine derivatives and related compounds as bcl-2 inhibitors for the treatment of neoplastic and autoimmune diseases 发明人:CHEN YI 权利人:NEWAVE PHARMACEUTICAL INC 摘要:The present invention relates to compounds of Formula (II) and more preferably to 1H-pyrrolo[2,3-b]pyridine derivatives of formula (III) and related compounds. The variables are defined in the claims. The compounds are BCL-2 inhibitors for treating neoplastic, autoimmune or neurodegenerative diseases. The present description discloses the synthesis of exemplary compounds as well as pharmacological data thereof (pages 61 to 72; examples 1 to 4; tables). An exemplary compound is e.g. 4-(4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl]piperazin-1-yl)-2-[methyl(1H-pyrrolo[2,3-b]pyridin-5-yl)phosphoroso]-N-[3-nitro-4-[(oxan-4-yl methyl)amino]benzenesulfonyl]benzamide (example 1).
专利号:US-2023119463-A1 优先权日:2019-12-27 标题 :1h-pyrrolo[2,3-b]pyridine derivatives as bcl-2 inhibitors for the treatment of neoplastic and autoimmune diseases 发明人:CHEN YI 权利人:NEWAVE PHARMACEUTICAL INC 摘要:The present invention relates to 1H-pyrrolo[2,3-b]pyridine derivatives and related compounds as BCL-2 inhibitors for treating neoplastic, autoimmune or neurodegenerative diseases. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 162 to 233; examples 1 to 8; table; compound examples cpd-1 to cpd-135; biological examples 1 to 4).
专利号:CN-104370905-B 优先权日:2014-10-22 标 题:Synthesis of Bcl-2 Inhibitor ABT-199
专利号:CN-104370905-A 优先权日:2014-10-22 标题:Synthesis of Bcl-2 Inhibitor ABT-199