📜Dicyclohexylammonium (E)-3-(4-((E)-2-(2-Chloro-4-Fluorophenyl)-1-(1-(Tetrahydro-2H-Pyran-2-yl)-1H-Indazol-5-yl)But-1-En-1-yl)Phenyl)Acrylate置于硫酸体系中,用 水,甲苯 用作溶剂,化学反应生成(E)-3-[4-[(E)-2-(2-氯-4-氟苯基)-1-(1H-吲唑-5-基)丁-1-烯-1-基]苯基]-2-丙烯酸 参考文献: Process For The Preparation Of (E)-3-(4-((E)-2-(2-Chloro-4-Fluorophenyl)-1-(1H-Indazol-5-yl)But-1-En-1-yl)Phenyl)Acrylic Acid[fr] Procédé Pour La Préparation D'Acide (E)-3-(4-((E)-2-(2-Chloro-4-Fluorophényl)-1-(1H-Indazol-5-yl)But-1-én-1-yl)Phényl)Acrylique 标题: Process For The Preparation Of (E)-3-(4-((E)-2-(2-Chloro-4-Fluorophenyl)-1-(1H-Indazol-5-yl)But-1-En-1-yl)Phenyl)Acrylic Acid[fr] Procédé Pour La Préparation D'Acide (E)-3-(4-((E)-2-(2-Chloro-4-Fluorophényl)-1-(1H-Indazol-5-yl)But-1-én-1-yl)Phényl)Acrylique 摘要:描述了一种用于制备雌激素受体调节化合物(E)-3-(4-((E)-2-(2-氯-4-氟苯基)-1-(1H-吲哚-5-基)丁-1-烯-1-基)苯基)丙烯酸(I)及其盐的方法,以及用于制备(I)的中间体.
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-2024174678-A1 优先权日:2020-06-30 标 题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds
专利号:WO-2024165901-A1 优先权日:2023-02-06 标题 :BENZO[b]SELENOPHENES AS NOVEL SELECTIVE ESTROGEN RECEPTOR MODULATORS 发明人:ARSENJANS PAVELS; PAEGLE EDGARS 权利人:LATVIAN INST ORGANIC SYNTHESIS 摘要:The present invention relates to a novel benzoselenophenes as anticancer agents by modulating estrogen receptor alpha (ERα) activity, as well as methods of their manufacturing and use in different pharmaceutical compositions for the treatment of various diseases and disorders by administration of such substances.
专利号:US-11780834-B2 优先权日:2018-06-21 标题:Solid forms of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3- yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol and processes for preparing fused tricyclic compounds comprising a substituted phenyl or pyridinyl moiety, including methods of their use 发明人:CHUNG CHEOL KEUN; XU JIE; IDING HANS; CLAGG KYLE; DALZIEL MICHAEL; FETTES ALEC; GOSSELIN FRANCIS; LIM NGIAP-KIE; MCCLORY ANDREW; ZHANG HAIMING; CHAKRAVARTY PAROMA; NAGAPUDI KARTHIK; ROBINSON SARAH 权利人:HOFFMANN LA ROCHE; GENENTECH INC 摘要:Provided herein are solid forms, salts, and formulations of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol, processes and synthesis thereof, and methods of their use in the treatment of cancer.
1: Shah N, Mohammad AS, Saralkar P, Sprowls SA, Vickers SD, John D, Tallman RM, Lucke-Wold BP, Jarrell KE, Pinti M, Nolan RL, Lockman PR. Investigational chemotherapy and novel pharmacokinetic mechanisms for the treatment of breast cancer brain metastases. Pharmacol Res. 2018 Jun;132:47-68. doi: 10.1016/j.phrs.2018.03.021. Epub 2018 Mar 28. 2: Chinnasamy K, Saravanan M, Poomani K. Evaluation of binding and antagonism/downregulation of brilanestrant molecule in estrogen receptor-α via quantum mechanics/molecular mechanics, molecular dynamics and binding free energy calculations. J Biomol Struct Dyn. 2020 Jan;38(1):219-235. doi: 10.1080/07391102.2019.1574605. Epub 2019 Apr 30. 63:102719. doi: 10.1016/j.redox.2023.102719. Epub 2023 May 16.
合成参考文献
参考文献:10.1016/j.bmcl.2015.09.074 摘要:Govek SP, Nagasawa JY, Douglas KL, Lai AG, Kahraman M, Bonnefous C, Aparicio AM, Darimont BD, Grillot KL, Joseph JD, Kaufman JA, Lee K, Lu N, Moon MJ, Prudente RY, Sensintaffar J, Rix PJ, Hager JH, Smith ND. Optimization of an indazole series of selective estrogen receptor degraders: Tumor regression in a tamoxifen-resistant breast cancer xenograft. Bioorganic & Medicinal Chemistry Letters. 2015 Nov;25(22):5163–7. doi: 10.1016/j.bmcl.2015.09.074.