CAS: 920113-03-7; Riviciclib Hydrochloride

该化合物是一种化学物质,属于聚合物类别或各种工业应用中使用的特定化合物类别,尽管分子重量,结构和物理特性等具体特征可能不同,但P276-00一类物质通常根据其稳定性,反应性和其他材料的兼容性进行评估,它们可能具有耐热性,化学品和水分等特性,适合用于涂层,粘合剂或密封剂;此外,此类物质的安全数据表提供了处理,储存和潜在危害方面的关键信息;必须查阅具体技术数据或管制文件,以了解其应用,安全措施和环境影响方面的详细资料;在使用化学物质时,始终确保遵守当地的规定.

结构式图片

物理性质

MSDS等安全信息

    上下游产品

    (+)-trans-2-(2-chloro-phenyl)-5,7-dihydroxy-8-(2-hydroxymethyl-1-methyl-pyrrolidin-3-yl)-chromen-4-one (+/-)-trans-[1-methyl-3-(2,4,6-trimethoxyphenyl)pyrrolidin-2-yl]methanol (-)-trans-[1-methyl-3-(2,4,6-trimethoxyphenyl)pyrrolidin-2-yl]methanol 15H23NO4*C18H14O8C15H23NO4*C18H14O8

    合成工艺路线路线简述

    • 合成目标产物 P276 主要起始原料 P276-00 (Free Base)
    • 920113-02-6 = 920113-03-7
      反应条件:1.1 Reagents: Hydrochloric Acid Solvents: Isopropanol,Water; Heated
      标题:Synergistic Combination Cyclin-Dependent Kinase (Cdk) Inhibitors And Antineoplastic Agents For Treatment Of Squamous Cell Carcinoma Of Head And Neck
      参考文献:World Intellectual Property Organization]

      920113-01-5 = 920113-03-7
      反应条件:1.1 Reagents: Pyridinium Chloride; 1.5 H,180 °C; 180 °C -> 25 °C1.2 Reagents: Sodium Carbonate Solvents: Methanol; Ph 10
      标题:Compounds For The Treatment Of Cancers Associated With Human Papillomavirus
      参考文献:World Intellectual Property Organization]

      = 920113-03-7 [标题:Reaction Conditions
      标题:Pyrrolidine Substitute Flavones For The Treatment Of Inflammatory Disorders
      参考文献:United States]

      920113-02-6 = 920113-03-7
      反应条件:1.1 Reagents: Hydrochloric Acid Solvents: Isopropanol,Water; Heated
      标题:Pyrrolidine Substituted Flavones For Treatment Of Renal Cystic Diseases
      参考文献:World Intellectual Property Organization]

      920113-01-5 = 920113-03-7
      反应条件:1.1 Reagents: Pyridinium Chloride; 1.5 H,180 °C; 180 °C -> 25 °C1.2 Reagents: Sodium Carbonate Solvents: Methanol; Ph 101.3 Reagents: Hydrochloric Acid Solvents: Isopropanol
      标题:Pharmaceutical Combination Of Paclitaxel And Cyclin-Dependent Kinase (Cdk) Inhibitors For Treatment Of Breast Cancer
      参考文献:World Intellectual Property Organization]

      920113-02-6 = 920113-03-7
      反应条件:1.1 Reagents: Hydrochloric Acid Solvents: Isopropanol,Water; Heated
      标题:Enantiomerically Pure Flavone Derivatives For The Treatment Of Proliferative Disorders And Processes For Their Preparation
      参考文献:World Intellectual Property Organization
    📜(+)-Trans-2-(2-Chloro-Phenyl)-5,7-Dihydroxy-8-(2-Hydroxymethyl-1-Methyl-Pyrrolidin-3-yl)-Chromen-4-One置于盐酸体系中,用 甲醇,异丙醇 作为反应溶剂,以92%的收率获得产物p276-00抑制剂
    参考文献: An Improved Process For Preparation Of An Intermediate Of The Pyrrolidine Substituted Flavones[fr] Procédé Amélioré Pour La Préparation D'Un Intermédiaire De Flavones Substituées Par Pyrrolidine
    标题: An Improved Process For Preparation Of An Intermediate Of The Pyrrolidine Substituted Flavones[fr] Procédé Amélioré Pour La Préparation D'Un Intermédiaire De Flavones Substituées Par Pyrrolidine
    摘要:本发明涉及一种用于制备一种关键中间体(如本文所述)的过程,该中间体用于合成嘧啶取代黄酮类化合物的(+)-反式对映体,该化合物由式(1)所表示,或其药学上可接受的盐;这些化合物是细胞周期依赖性激酶(cdks)的抑制剂,可用于治疗癌症等增殖性疾病.式(1)中r1的含义如索引中所示.本发明的过程具有较高的产率和纯度优势,反应温度较低,一致性好,并且使用无毒溶剂.本发明的过程允许高效的大规模合成,所得产品的纯度大于97%.

    海关参考信息

    专利信息


    专利号:US-7951961-B2
    优先权日:2006-07-07
    标题:Enantioselective synthesis of pyrrolidines substituted with flavones, and intermediates thereof
    发明人：SIVAKUMAR MEENAKSHI; SHUKLA MANOJ; JADHAV PRAMOD KUMAR; BORHADE AJIT
    权利人:PIRAMAL LIFE SCIENCES LTD
    摘要:The present invention relates to an enantioselective synthesis of (+)-trans enantiomer of pyrrolidines substituted with flavones, represented by Formula 1 or salts thereof, which are inhibitors of cyclin dependant kinases and can be used for treatment of proliferative disorders such as cancer n nwherein Ar has the meaning as indicated in the claims.

    专利号:WO-2014128524-A1
    优先权日:2013-02-19
    标题:An improved process for preparation of an intermediate of the pyrrolidine substituted flavones
    发明人：CHENNAMSETTY SUNEELMANOHARBABU; PATIL RAJENDRA; HAREL PRASHANT; HARIHARAN SIVARAMAKRISHNAN
    权利人:PIRAMAL ENTPR LTD
    摘要:The present invention relates to a process for the preparation of a key intermediate (as described herein) used in the synthesis of (+)- trans enantiomer of pyrrolidine substituted flavones, represented by the compounds of formula (1) or pharmaceutically acceptable salts thereof; which are inhibitors of cyclin dependant kinases (CDKs) and can be used in the treatment of proliferative disorders such as cancer. Formula (1) wherein R 1 has the meaning as indicated in the claims. The process of the present invention has advantages of higher yield and purity, lower reaction temperature, is consistent and involves the use of non toxic solvents. The process of the present invention allows efficient large-scale synthesis and purity of the product obtained is greater than 97 %.

    专利号:WO-2014128523-A1
    优先权日:2013-02-19
    标 题 :A process for preparation of an intermediate of the pyrrolidine substituted flavones
    发明人：CHENNAMSETTY SUNEELMANOHARBABU; BOKKA RAVISHANKAR; VEERAPPAN RATHINASAMI; SIVAKUMAR MEENAKSHI; HARIHARAN SIVARAMAKRISHNAN
    权利人:PIRAMAL ENTPR LTD
    摘要:The present invention relates to a process for the preparation of a key intermediate (as described herein) used in the synthesis of (+)- trans enantiomer of pyrrolidine substituted flavones, represented by the compounds of formula (1) or pharmaceutically acceptable salts thereof; which are inhibitors of cyclin dependant kinases (CDKs) and can be used in the treatment of proliferative disorders such as cancer. Formula (1) wherein R has the meaning as indicated in the claims. The process of the present invention has advantages of higher yield and purity, lower reaction temperature, is consistent and involves the use of non toxic solvents. The process of the present invention allows efficient large-scale synthesis and purity of the product obtained is greater than 97 %.

    专利号:AU-2006346193-A2
    优先权日:2006-07-07
    标 题:An enantioselective synthesis of pyrrolidine-substituted flavones

    专利号:AU-2006346193-C1
    优先权日:2006-07-07
    标题:An enantioselective synthesis of pyrrolidine-substituted flavones

    专利号:AU-2006346193-B2
    优先权日:2006-07-07
    标题 :An enantioselective synthesis of pyrrolidine-substituted flavones

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    主要参考文献


    1: Shirsath N, Rathos M, Chaudhari U, Sivaramakrishnan H, Joshi K. Potentiation of anticancer effect of valproic acid, an antiepileptic agent with histone deacetylase inhibitory activity, by the cyclin-dependent kinase inhibitor P276-00 in human non-small-cell lung cancer cell lines. Lung Cancer. 2013 Nov;82(2):214-21. doi: 10.1016/j.lungcan.2013.08.010. Epub 2013 Sep 3. doi: 10.1186/1479-5876-11-42.
    3: Rathos MJ, Khanwalkar H, Joshi K, Manohar SM, Joshi KS. Potentiation of in vitro and in vivo antitumor efficacy of doxorubicin by cyclin-dependent kinase inhibitor P276-00 in human non-small cell lung cancer cells. BMC Cancer. 2013 Jan 23;13:29. doi: 10.1186/1471-2407-13-29.
    4: Shirsath NP, Manohar SM, Joshi KS. P276-00, a cyclin-dependent kinase inhibitor, modulates cell cycle and induces apoptosis in vitro and in vivo in mantle cell lymphoma cell lines. Mol Cancer. 2012 Oct 18;11:77. doi: 10.1186/1476-4598-11-77.

    合成参考文献


    参考文献:10.1016/j.bmc.2023.117561
    摘要:Takarada JE, Cunha MR, Almeida VM, Vasconcelos SNS, Santiago AS, Godoi PH, Salmazo A, Ramos PZ, Fala AM, de Souza LR, Da Silva IEP, Bengtson MH, Massirer KB, Couñago RM. Discovery of pyrazolo[3,4-d]pyrimidines as novel mitogen-activated protein kinase kinase 3 (MKK3) inhibitors. Bioorg Med Chem. 2024 Jan 15;98():117561. doi: 10.1016/j.bmc.2023.117561.
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