CAS: 1001264-89-6; (S)-2-(4-Chlorophenyl)-1-(4-((5R,7R)-7-Hydroxy-5-Methyl-6,7-Dihydro-5H-Cyclopenta[d]Pyrimidin-4-yl)Piperazin-1-yl)-3-(Isopropylamino)Propan-1-One

该化合物是一个小分子抑制器,主要针对蛋白质动脉AKT,它在各种细胞过程中,包括新陈代谢,扩散和生存过程中发挥着关键作用;该化合物在癌症研究中尤其重要,因为AKT的异常信号往往与肿瘤生长和抗药性有关;GDC-0068显示AKT的血型具有很高的选择性,使其成为研究AKT信号路径及其对发酵的影响的宝贵工具;该物质的特点通常是能够抑制AKT磷酸盐,从而破坏下游信号路径,从而助长癌症细胞生存和扩散;在临床研究中,GDC-0068显示有望提高其他抗癌剂的功效,表明其作为综合疗法的潜力;其药性特性,包括吸收,分布,新陈代谢和排泄,对于确定其临床应用中的治疗窗口和安全特征至关重要;

结构式图片

上下游产品

Tert-Butyl ((S)-2-(4-Chlorophenyl)-3-(4-((5R,7R)-7-Hydroxy-5-Methyl-6,7-Dihydro-5H-Cyclopenta[d]Pyrimidin-4-yl)Piperazin-1-yl)-3-Oxopropyl)(Isopropyl)Carbamate 1001270-64-9
Tert-Butyl 4-((5R,7R)-7-Hydroxy-5-Methyl-6,7-Dihydro-5H-Cyclopenta[d]Pyrimidin-4-yl)Piperazine-1-Carboxylate 1001180-45-5
Tert-Butyl 4-((5R)-7-Hydroxy-5-Methyl-6,7-Dihydro-5H-Cyclopenta[d]Pyrimidin-4-yl)-Piperazine-1-Carboxylate 1001180-18-2
Tert-Butyl 4-((5R,7R)-5-Methyl-7-((4-Nitrobenzoyl)Oxy)-6,7-Dihydro-5H-Cyclopenta[d]Pyrimidin-4-yl)-Piperazine-1-Carboxylate 1001180-47-7
(R)-4-(5-甲基-7-氧代-6,7-二氢-5H-环戊烷并[d]嘧啶-4-基)哌嗪-1-羧酸叔丁酯 (R)-Tert-Butyl 4-(5-Methyl-7-Oxo-6,7-Dihydro-5H-Cyclopenta[d]Pyrimidin-4-yl)Piperazine-1-Carboxylate 1001180-21-7
(R)-Tert-Butyl 4-(6-Chloro-5-(4-Methoxy-4-Oxobutan-2-yl)Pyrimidin-4-yl)Piperazine-1-Carboxylate

合成工艺路线路线简述

    Methyl 2-(4-Chlorophenyl)Acrylate置于盐酸,Lithium Hydroxide,正丁基锂,水,双氧水,N,N-二异丙基乙胺体系中,用 四氢呋喃,1,4-二氧六环,Hexanes,二氯甲烷 用作溶剂,化学反应 5.17H,反应生成帕他色替
    参考文献:Wo2008/6040
    标题:Wo2008/6040

    海关参考信息

    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-2025289827-A1
    优先权日:2022-12-02
    标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
    发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
    权利人:C4 THERAPEUTICS INC
    摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

    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: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.

    专利号:AR-124856-A2
    优先权日:2014-09-26
    标题 :PROCESS FOR PREPARING AN INTERMEDIATE COMPOUND FOR THE SYNTHESIS OF (CYCLOPENTYL[D]PYRIMIDIN-4-IL)PIPERAZINE COMPOUNDS

    专利号:US-2022047711-A1
    优先权日:2018-12-10
    标题 :Photocrosslinking peptides for site specific conjugation to fc-containing proteins
    发明人:SADOWSKY JACK; ZACHARIAS NEELIE TYANA
    权利人:GENENTECH INC
    摘要:Provided herein are peptides having a photocrosslinking moiety useful for the synthesis of antibody-drug conjugates as well as methods of making and using such conjugates.
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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Lin J, Sampath D, Nannini MA, Lee BB, Degtyarev M, Oeh J, Savage H, Guan Z, Hong R, Kassees R, Lee LB, Risom T, Gross S, Liederer BM, Koeppen H, Skelton NJ, Wallin JJ, Belvin M, Punnoose E, Friedman LS, Lin K. Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models. Clin Cancer Res. 2013 Apr 1;19(7):1760-72. doi: 10.1158/1078-0432.CCR-12-3072. doi: 10.1158/1078-0432.CCR-13-0978. doi: 10.1126/scisignal.2005125.
    6: Wehrenberg-Klee E, Turker NS, Heidari P, Larimer B, Juric D, Baselga J, Scaltriti M, Mahmood U. Differential Receptor Tyrosine Kinase PET Imaging for Therapeutic Guidance. J Nucl Med. 2016 Sep;57(9):1413-9. doi: 10.2967/jnumed.115.169417. doi: 10.1158/2159-8290.CD-16-0512.
    9: Yang G, Murashige DS, Humphrey SJ, James DE. A Positive Feedback Loop between Akt and mTORC2 via SIN1 Phosphorylation. Cell Rep. 2015 Aug 11;12(6):937-43. doi: 10.1016/j.celrep.2015.07.016.

    合成参考文献


    参考文献:10.1038/s41392-021-00522-6
    摘要:Xie Q, Chi S, Fang Y, Sun Y, Meng L, Ding J, Chen Y. PI3Kα inhibitor impairs AKT phosphorylation and synergizes with novel angiogenesis inhibitor AL3810 in human hepatocellular carcinoma. Signal Transduction and Targeted Therapy. 2021 Mar 31;6(1):130. doi: 10.1038/s41392-021-00522-6.
    参考文献:10.1016/j.bbrc.2022.03.029
    摘要:Hu C, Shang X, Zheng T, Hu X, Zhao Y. Ipatasertib (GDC-0068) and erdafitinib co-treatment for inducing mitochondrial apoptosis through Bim upregulation in bladder cancer cells. Biochemical and Biophysical Research Communications. 2022 May;604():165–71. doi: 10.1016/j.bbrc.2022.03.029.
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