CAS: 1198300-79-6; 4-(Cyclopropylamino)-2-((4-(4-(Ethylsulfonyl)Piperazin-1-yl)Phenyl)Amino)Pyrimidine-5-Carboxamide

该化合物是合成有机化合物,其特征是其复杂的分子结构,包括一种与各种功能组的替代的丙基,其中含有一种火利米丁核.该化合物的特性是环丙基氨基和一种管子动物,表明它与生物目标可能发生相互作用,特别是在药理学方面.乙基磺酰基组的存在表明溶性和生物利用率提高,这对于治疗应用至关重要.该化合物的结构意味着它可能具有酶抑制或感应调节等特性,从而成为药物开发的候选物.其具体特性,包括熔点,溶性,溶性,稳定性,将取决于分子相互作用和研究的环境.

结构式图片

合成工艺路线路线简述

    4-Cyclopropylamino-2-(Methylsulfanyl)Pyrimidine-5-Carboxylic Acid Ethyl Ester置于sodium Ethanolate,Formamide,间氯过氧苯甲酸体系中,用 N-甲基吡咯烷酮,N,N-二甲基甲酰胺 用作溶剂,化学反应 23.28H,反应生成赛度替尼
    参考文献:Wo2019213606A5
    标题:Wo2019213606A5

    海关参考信息

    专利信息


    专利号:US-2025206743-A1
    优先权日:2022-03-25
    标 题:Tyk2 inhibitor synthesis and intermediates thereof
    发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
    权利人:TAKEDA PHARMACEUTICALS CO
    摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

    专利号:US-12441733-B2
    优先权日:2018-03-26
    标题:Substituted 2,4-dioxotetrahydropyrimidines as intermediates in the synthesis of bruton's tyrosine kinase inhibitors
    发明人:ARISTA LUCA; HEBACH CHRISTINA; HOLLINGWORTH GREGORY JOHN; HOLZER PHILIPP; IMBACH-WEESE PATRICIA; LORBER JULIEN; MACHAUER RAINER; SCHMIEDEBERG NIKO; VULPETTI ANNA; ZOLLER THOMAS
    权利人:NOVARTIS AG
    摘要:The invention relates to compounds of the formulae (I), (III), (IIIa), (XXIa), (XXIII), and/or (XLVI)or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

    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-11339145-B2
    优先权日:2018-05-04
    标题 :Synthesis of cerdulatinib
    发明人:PANDEY ANJALI; SRAN ARVINDER; CHEN YING; POGGIALI DANIELE; FUMAGALLI TIZIANO
    权利人:ALEXION PHARMA INC
    摘要:The present disclosure provides processes for the preparation of cerdulatinib, which is of formula I:or a salt thereof. The disclosure also provides intermediates and processes for the preparation of the intermediates useful in the preparation of cerdulatinib or a salt thereof.

    专利号:US-10906888-B2
    优先权日:2016-07-14
    标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme
    发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE
    权利人:PFIZER
    摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

    专利号:US-2019337930-A1
    优先权日:2018-05-04
    标 题 :Synthesis of cerdulatinib
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    主要参考文献


    1: Traidl S, Freimooser S, Werfel T. Janus kinase inhibitors for the therapy of atopic dermatitis. Allergol Select. 2021 Aug 27;5:293-304. doi: 10.5414/ALX02272E.
    2: Montilla AM, Gómez-García F, Gómez-Arias PJ, Gay-Mimbrera J, Hernández-Parada J, Isla-Tejera B, Ruano J. Scoping Review on the Use of Drugs Targeting JAK/STAT Pathway in Atopic Dermatitis, Vitiligo, and Alopecia Areata. Dermatol Ther (Heidelb). 2019 Dec;9(4):655-683. doi: 10.1007/s13555-019-00329-y. Epub 2019 Oct 13.
    3: Coffey GP, Feng J, Betz A, Pandey A, Birrell M, Leeds JM, Der K, Kadri S, Lu P, Segal J, Wang YL, Michelson G, Curnutte JT, Conley PB. Cerdulatinib Pharmacodynamics and Relationships to Tumor Response Following Oral Dosing in Patients with Relapsed/Refractory B-cell Malignancies. Clin Cancer Res. 2019 Feb 15;25(4):1174-1184. doi: 10.1158/1078-0432.CCR-18-1047. Epub 2018 Oct 17. 6(41):43881-96. doi: 10.18632/oncotarget.6316.

    合成参考文献


    参考文献:10.1038/s41571-019-0239-8
    摘要:Bosch F, Dalla-Favera R. Chronic lymphocytic leukaemia: from genetics to treatment. Nature Reviews Clinical Oncology. 2019 Jul 05;16(11):684–701. doi: 10.1038/s41571-019-0239-8.
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