CAS: 1532533-67-7; (S)-2-(1-(4-Amino-3-(3-Fluoro-4-Isopropoxyphenyl)-1H-Pyrazolo[3,4-D]Pyrimidin-1-yl)Ethyl)-6-Fluoro-3-(3-Fluorophenyl)-4H-Chromen-4-One

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    专利号:US-11891375-B2
    优先权日:2021-07-26
    标 题 :Method for the synthesis of 2,4-dimethylpyrimidin-5-ol, intermediates, and method for the synthesis of Lemborexant using the intermediates
    发明人:AKHATOU ABDESLAM; DOBARRO RODRÃ?GUEZ ALICIA
    权利人:MOEHS IBERICA SL
    摘要:A method is for the synthesis of 2,4-dimethylpyrimidin-5-ol, which can be used as an intermediate compound in the synthesis of Lemborexant. The method includes reacting a nitrophenyl compound with N,N-dimethylformamide diethyl acetal.

    专利号:EP-1246837-B1
    优先权日:2000-01-11
    标 题:Oligomers of nonpeptide restricted mimetics of dipeptides or tripeptides and the use thereof in the synthesis of synthetic proteins and polypeptides
    发明人:AMBLARD MURIEL; MARTINEZ JEAN; BERGE GILBERT
    权利人:CENTRE NAT RECH SCIENT
    摘要:The invention relates to nonpeptide oligomers of amino acids. The oligomers comprise -(NR'-A-CO)-O- units which represent a nonpeptide, restricted-mimetic inducer of the beta turn in a dipeptide or tripeptide fragment. Said oligomers may be produced by peptide synthesis techniques, whether in solution or in the solid phase, and can be used in the synthesis of synthetic proteins or polypeptides, in which the peptide fragment(s) (is) are identical to those of the corresponding natural protein or polypeptide and whose structural fragment(s) comprise(s) a fragment of an oligomer according to the invention.

    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-9499643-B2
    优先权日:2010-01-08
    标题 :Method for preparing carbene in solution, novel stable form of carbene obtained in particular by means of said method, and uses thereof in catalysis
    发明人:MALIVERNEY CHRISTIAN; SAINT-JALMES LAURENT; GOJON SOPHIE; KATO TSUYOSHI; BACEIREDO ANTOINE J
    权利人:MALIVERNEY CHRISTIAN; SAINT-JALMES LAURENT; GOJON SOPHIE; KATO TSUYOSHI; BACEIREDO ANTOINE J; BLUESTAR SILICONES FRANCE; CENTRE NAT RECH SCIENT
    摘要:The invention relates to a method for preparing carbene by means of deprotonation of a precursor salt using a strong base. A purpose of the invention is to enhance the synthesis of carbenes, i.e. to simplify same, to make said synthesis more economical and to obtain a liquid or solid, stable and pure form constituting a catalytic system that is easy to store and use and that has a higher efficiency, higher yield and higher selectivity than carbene catalysts of the prior art. In order to do so, the method comprises deprotonation in a solvent including an alcohol. The invention also relates to an alcohol-containing solution and carbene, and to a solid that can be obtained from the solution, e.g. by means of sublimation.

    专利号:US-11542244-B2
    优先权日:2018-05-18
    标题 :Synthesis of tipifarnib
    发明人:REN PINGDA; DENG XIAOHU; MAI WANPING
    权利人:KURA ONCOLOGY INC
    摘要:Provided herein are methods of preparing a desired enantiomer 6-[amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl) methyl]-4-(3-chlorophenyl)-1-methyl-2(1H)-quinolinone, otherwise known as tipifarnib.

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    主要参考文献


    1: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Umbralisib. 2023 Oct 10. 81(7):857-866. doi: 10.1007/s40265-021-01504-2. 78(12):1018-1020. doi: 10.1093/ajhp/zxab117. 23(5):535-541. doi: 10.1080/14656566.2022.2043273. Epub 2022 Feb 24. 9(6):OF5. doi: 10.1158/2159-8290.CD-NB2019-045. Epub 2019 Apr 1. 122(6):23. doi: 10.1097/01.NAJ.0000833916.26417.b5. 39(15):1609-1618. doi: 10.1200/JCO.20.03433. Epub 2021 Mar 8.
    8: Proudman D, Nellesen D, Gupta D, Adib D, Yang J, Mamlouk K. A Matching- Adjusted Indirect Comparison of Single-Arm Trials in Patients with Relapsed or Refractory Follicular Lymphoma Who Received at Least Two Prior Systemic Treatments: Tazemetostat was Associated with a Lower Risk for Safety Outcomes Versus the PI3-Kinase Inhibitors Idelalisib, Duvelisib, Copanlisib, and Umbralisib. Adv Ther. 2022 Apr;39(4):1678-1696. doi: 10.1007/s12325-022-02054-z. Epub 2022 Feb 14.
    9: Bajaj S, Barrett SM, Nakhleh RE, Brahmbhatt B, Bi Y. Umbralisib-Induced Immune-Mediated Colitis: A Concerning Adverse Effect of the Novel PI3Kδ/CK1ε Inhibitor. ACG Case Rep J. 2021 Nov 24;8(11):e00701. doi: 10.14309/crj.0000000000000701.

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