CAS: 1489389-18-5; (R)-5-((4-((Morpholin-2-Ylmethyl)Amino)-5-(Trifluoromethyl)Pyridin-2-yl)Amino)Pyrazine-2-Carbonitrile

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合成工艺路线路线简述

    📜2-氨基-5-氰基吡嗪置于(S,R)-Ppf-P(T-Bu)2,碘代三甲硅烷,Palladium Diacetate体系中,用 水,N,N-二甲基甲酰胺,乙腈 用作溶剂,化学反应 4.0H,反应生成Cct245737游离态
    参考文献: Methods For Synthesis Of Chk1 Inhibitors[fr] Méthodes De Synthèse D'Inhibiteurs De Chk1
    标题: Methods For Synthesis Of Chk1 Inhibitors[fr] Méthodes De Synthèse D'Inhibiteurs De Chk1
    摘要:目前的技术涉及到用于偶联反应的过程,化合物,组合物和方法.此外,本公开提供了与chk1抑制剂sra737相关的新型中间体,物质组合物和过程.

    海关参考信息

    专利信息


    专利号:US-2023150994-A1
    优先权日:2020-04-07
    标 题:Methods for synthesis of chk1 inhibitors
    发明人:SCHWAEBE MICHAEL; ROSNER THORSTEN; ZHAO DALIAN; MILLER ROSS; DULINA RICH; HUMORA MICHAEL; GOTTSCHLING STEPHEN E
    权利人:SIERRA ONCOLOGY INC
    摘要:The present technology relates to processes, compounds, compositions, and methods useful for coupling reactions. Also, the present disclosure provides for novel intermediates, compositions of matter, and processes relating to the Chk1 inhibitor, SRA737.

    专利号:TW-202204348-A
    优先权日:2020-04-07
    标 题:Methods for synthesis of chk1 inhibitors

    专利号:EP-4132922-A1
    优先权日:2020-04-07
    标 题 :Methods for synthesis of chk1 inhibitors

    专利号:WO-2021207210-A1
    优先权日:2020-04-07
    标 题 :Methods for synthesis of chk1 inhibitors

    专利号:WO-2023226658-A1
    优先权日:2022-05-25
    标题:Nitrogen-containing five-membered heterocyclic derivatives as checkpoint kinase 1 inhibitor and uses thereof
    发明人:LIU HANLAN; MA JINGJING; HUANG YUNG-JEN; CAI ZHANG; WANG XIAOHUI; YAN ZHIYU; KHAN PASHA M; PANPATIL DAYANAND; PUJALA BRAHMAM; RUAN JUXIN
    权利人:SPEROGENIX THERAPEUTICS LTD
    摘要:The present disclosure relates generally to nitrogen-containing five-membered heterocyclic derivatives usefulness in treatment of conditions associated with Checkpoint kinase (CHK), particularly more specifically CHK-1 enzymes. Methods of use, compositions, and method of synthesis are also disclosed.

    专利号:US-12428395-B2
    优先权日:2019-08-01
    标题 :Heterocyclic compounds as kinase inhibitor and uses thereof
    发明人:PENDHARKAR DHANANJAY; RAMACHANDRAN SREEKANTH A; JADHAVAR PRADEEP S; PANPATIL DAYANAND; SAEED UZMA; KUMAR VIVEK; BIST DIPSHE
    权利人:SPEROGENIX THERAPEUTICS LTD
    摘要:The present disclosure relates generally to compounds useful in treatment of conditions associated with Checkpoint kinase (CHK), particularly CHK-1 enzymes. Specifically, the present invention discloses compound of formula (IA), which exhibits inhibitory activity against CHK-1 enzymes. Methods of treating conditions associated with excessive activity of CHK-1 enzymes with such compounds is disclosed. Uses thereof, pharmaceutical compositions, kits and method of synthesis also disclosed.

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    ✅ COA系统入驻 | 共享模式

    主要参考文献

    Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737) James D. Osborne, Thomas P. Matthews, Tatiana McHardy, Nicolas Proisy, Kwai-Ming J. Cheung, Michael Lainchbury, Nathan Brown, Michael I. Walton, Paul D. Eve, Katherine J. Boxall, Angela Hayes, Alan T. Henley, Melanie R. Valenti, Alexis K. De Haven Brandon, Gary Box, Yann Jamin, Simon P. Robinson, Isaac M. Westwood, Rob L. M. van Montfort, Philip M. Leonard, Marieke B. A. C. Lamers, John C. Reader, G. Wynne Aherne, Florence I. Raynaud, Suzanne A. Eccles, Michelle D. Garrett, and Ian Collins Publication Date (Web): May 11, 2016 (Article) DOI: 10.1021/acs.jmedchem.5b01938

    合成参考文献


    参考文献:10.1016/j.ejmech.2018.03.075
    摘要:Tian C, Han Z, Li Y, Wang M, Yang J, Wang X, Zhang Z, Liu J. Synthesis and biological evaluation of 2,6-disubstituted-9H-purine, 2,4-disubstitued-thieno[3,2-d]pyrimidine and -7H-pyrrolo[2,3-d]pyrimidine analogues as novel CHK1 inhibitors. European Journal of Medicinal Chemistry. 2018 May;151():836–48. doi: 10.1016/j.ejmech.2018.03.075.
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