CAS: 847818-55-7; (1-Methyl-1H-Pyrazol-4-yl)Boronic Acid

该化合物是一种有机有机体化合物,其特征是配有一种附于丙烯环上的黄酸功能组,该化合物一般显示白色至白色表面的固体外观,可溶于水和酒精等极地溶剂中,由于它能够形成氢结核,这是boronic酸的一个常见特征.阳极酸的存在有助于其潜在的再活性,特别是在铃木的组合反应中,使其在有机合成和药用化学中具有价值.该泡沫酸组允许与二醇形成可逆的共价结合,这对生物应用,包括药物设计和开发具有重要意义.此外,该化合物可能展示出有趣的生物活动,尽管具体的生物特性取决于其使用的背景.总体来说,(1-M乙基-1H-Pyrazol-4-yyyl)boronoron酸是合成化学中的一种多用途建筑,特别是在制药和农用化学的开发中.

结构式图片

相似化合物

761446-44-0 1022151-50-3 1188405-87-9

欧盟法规

C&L通报

上下游产品

CAS号15803-02-8 4-溴-1-甲基-1H-吡唑 | CAS号930-36-9 1-甲基吡唑 | CAS号761446-44-0 1-甲基吡唑-4-硼酸频哪醇酯

合成工艺路线路线简述

  • 合成目标产物 1-Methyl-1H-Pyrazole-4-Boronic Acid 主要起始原料 4-Bromo-1-Methylpyrazole And Bis(Pinacolato)Diboron
  • 15803-02-8 = 847818-55-7
    反应条件:1.1 Reagents: Butyllithium Solvents: Tetrahydrofuran,Hexane; -90 °C; < -80 °C; 1 H,-90 °C1.2 Reagents: Trimethyl Borate; 0.5 H,-70 °C; -70 °C -> -15 °C1.3 Reagents: Ammonium Chloride Solvents: Water; Neutralized,-15 °C; -15 °C -> Rt; 1 H,Rt
    标题:Synthesis Of Pinacol Esters Of 1-Alkyl-1H-Pyrazol-5-Yl- And 1-Alkyl-1H-Pyrazol-4-Ylboronic Acids
    作者:Ivachtchenko,Alexandre V.; Kravchenko,Dmitry V.; Zheludeva,Valentina I.; Pershin,Dmitry G.
    参考文献:Journal Of Heterocyclic Chemistry 日期:2004 卷标:41(6) 页码:931-939]

    1173889-20-7 = 847818-55-7
    反应条件:1.1 Reagents: Ammonium Hydroxide Solvents: Methanol,Water; > 15 Min,Rt
    标题:Synthesis Of The Hydrazinyl Pyridine Intermediate: Phase-Appropriate Delivery
    作者:Wilsily,Ashraf; Mennen,Steven M.; Cosbie,Andrew; Milne,Jacqueline E.
    参考文献:Organic Process Research & Development 日期:2017 卷标:21(9) 页码:1286-1293]

    15803-02-8 = 847818-55-7
    反应条件:1.1 Reagents: Butyllithium Solvents: Tetrahydrofuran; -90 °C1.2 Reagents: Trimethyl Borate; -90 °C
    标题:Process Development And Large-Scale Synthesis Of A C-Met Kinase Inhibitor
    作者:Stewart,Gavin W.; Brands,Karel M. J.; Brewer,Sarah E.; Cowden,Cameron J.; Davies,Antony J.; Et Al
    参考文献:Organic Process Research & Development 日期:2010 卷标:14(4) 页码:849-858]

    15803-02-8 = 847818-55-7
    反应条件:1.1 Reagents: Butyllithium Solvents: Tetrahydrofuran; -90 °C1.2 Reagents: Trimethyloxonium Tetrafluoroborate; -90 °C1.3 Reagents: Ammonium Chloride; -90 °C
    标题:An Improved Synthesis Of 1-Methyl-1H-Pyrazole-4-Boronic Acid Pinacol Ester And Its Corresponding Lithium Hydroxy Ate Complex: Application In Suzuki Couplings
    作者:Mullens,Peter R.
    参考文献:Tetrahedron Letters 日期:2009 卷标:50(49) 页码:6783-6786
1-甲基-4-溴吡唑置于正丁基锂,硼酸三甲酯,Ammonium Chloride体系中,用 四氢呋喃,正己烷 作为反应溶剂,化学反应 2.5H,以38%的收率获得产物1-甲基-1H-吡唑-4-硼酸
参考文献:1-烷基-1 H-吡唑-5-基和1烷基-1 H-吡唑-4-基硼酸频哪醇酯的合成
标题:1-烷基-1 H-吡唑-5-基和1烷基-1 H-吡唑-4-基硼酸频哪醇酯的合成
摘要:从1 H-吡唑开始,合成并表征了多种1-烷基-1 H-吡唑-4-基和1-烷基-1 H-吡唑-5-基硼酸及其频哪醇酯.所述方法中的关键步骤是吡唑环的区域选择性锂化.合成的松果酸酯在长期保存下是稳定的,可以用作有机合成中的方便试剂.
DOI:10.1002/jhet.5570410612

专利信息


专利号:EP-3567040-B1
优先权日:2013-06-24
标 题 :Method for the preparation of intermediates useful for the synthesis of [1,2,4]-triazolo[4,3-a]pyridines

专利号:WO-2023091726-A1
优先权日:2021-11-18
标题:Inhibitors of cyclin‑dependent kinase 12 (cdk12)
发明人:BENOIT GUILLAUME; CARULLI JOHN; CHEN FEI; CHUAQUI CLAUDIO; CIBLAT STEPHANE; COOPER ELLIOT; DAGENAIS ROBIN; HU SHANHU; KABRO ANZHELIKA; LAPLACA DEREK; MARINEAU JASON; MOEBIUS DAVID; MOON DIANE; SOLODININ ANDREI; WHITMORE KENNETH
权利人:SYROS PHARMACEUTICALS INC
摘要:The present invention provides chemical compounds that inhibit one or more families of kinases (e.g., serine/threonine kinases, including one or more of the families of CDK proteins, and in particular, CDK12). More specifically, the present invention provides CDK12 inhibitors, of formula (I), pharmaceutically acceptable salts and isotopically labeled derivatives thereof, pharmaceutical compositions containing the compounds/inhibitors, and methods of their synthesis and use in treating proliferative diseases (e.g., a bladder cancer, a breast cancer, Ewing's sarcoma, a gastric cancer, a gastrointestinal cancer, a hematologic cancer, a lung cancer (e.g., small cell lung cancer (SCLC)), an ovarian cancer (e.g., a high grade serous ovarian cancer), a pancreatic cancer (e.g., pancreatic ductal adenocarcinoma (PDAC)), a brain cancer (e.g., glioblastoma), or a prostate cancer), alone or in combination with a second therapeutic agent. The proliferative disease can be a cancer, benign neoplasm, or pathologic angiogenesis, and any of the therapeutic methods or uses described herein can include a step of diagnosing the patient's disease. In other embodiments of the invention, the compositions described herein (e.g., the compounds, pharmaceutical compositions, and kits containing them) are used for the treatment of myotonic dystrophy (type 1 or type 2).

专利号:US-2022204495-A1
优先权日:2019-05-03
标题:Inhibiting trabid
发明人:CAMPBELL ANNE-MARIE; MARCIN Lawrence; KAYSER-BRICKER KATHERINE
权利人:VALO HEALTH INC; INTEGRAL HEALTH HOLDINGS LLC
摘要:The present disclosure is directed to compounds of formulas (I)-(VII), which are useful as modulators of TRABID. The compounds are further useful in the inhibition of TRABID and the treatment of diseases or disorders associated with the inhibition of TRABID. For instance, the disclosure is concerned with compounds and compositions for inhibition of TRABID, methods of treating diseases associated with the inhibition of TRABID (e.g., autoimmune inflammatory diseases including, but not limited to, psoriasis), and methods of synthesis of these compounds.

专利号:EP-3567040-A1
优先权日:2013-06-24
标题 :Method for the preparation of intermediates useful for the synthesis of [1,2,4]-triazolo[4,3-a]pyridines

专利号:WO-2022162606-A1
优先权日:2021-01-30
标 题:Heterocyclic compounds as kinase inhibitor and uses thereof
发明人:YAN ZHIYU; WANG XIAOHUI; LIU HANLAN; KHAN PASHA M; PANPATIL DAYANAND; PUJALA BRAHMAM; PENDHARKAR DHANANJAY; JADHAVAR PRADEEP S; SAEED UZMA; KUMAR VIVEK
权利人:SPEROGENIX THERAPEUTICS LTD; INTEGRAL BIOSCIENCES PRIVATE 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 (J), which exhibits inhibitory activity against CHK-1 enzymes. Methods of treating conditions associated with excessive activity of CHK-1 enzymes such as cancer, idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) with such compounds is disclosed. Uses thereof, pharmaceutical compositions, kits and method of synthesis also disclosed. Formula (J)
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合成参考文献


摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 175.
摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 199.
摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 102.
摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2026).
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