CAS: 56423-63-3; 2-Bromopyrazine

该化合物是一种杂交化合物,其特点是在2位置用溴原子取代了一条双子环,这种多用途中间体广泛用于制药和农用化学合成,因为它在交叉反应中具有反应性,如铃木-宫浦和Buchwald-Hartwig的结合.其电子衰弱的双子体核心会增加电益替代,使其对建设复杂的双环框架很有价值.溴替代体是进一步功能化的处理器,能够进行精确的修改.在标准条件下,高纯度和稳定性的2-Bromopyrazine是研究和工业应用的可靠建筑块.它与各种反应条件的兼容性强调了其在医药化学和材料科学中的实用性.

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23229-26-7 23229-25-6 95538-03-7

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CAS号6270-63-9 羟基吡嗪 | CAS号14508-49-7 2-氯吡嗪 | CAS号30882-41-8 pyrazine hydr°C... | CAS号290-37-9 吡嗪 | CAS号7732-18-5 水 | CAS号7726-95-6 溴素 | CAS号108030-81-5 2-(4-甲氧基苯基)吡嗪 | CAS号95538-03-7 2,3-二溴吡嗪 | CAS号23229-25-6 2,6-二溴吡嗪 | CAS号23229-26-7 2,5-二溴吡嗪 | CAS号19847-12-2 2-氰基吡嗪 | CAS号29460-97-7 2-苯基吡嗪 | CAS号56421-72-8 2-噻吩-2-吡嗪

合成工艺路线路线简述

    📜2-氯吡嗪置于三甲基溴硅烷体系中,用 Various Solvent(S) 作为反应溶剂,化学反应 50.0H,以30%的收率获得产物2-溴吡嗪
    参考文献:吡啶和其他杂环中甲硅烷基介导的卤素/卤素置换
    标题:吡啶和其他杂环中甲硅烷基介导的卤素/卤素置换
    摘要:用溴三甲基硅烷加热将 2-氯吡啶转化为 2-溴吡啶,将 2-氯-6-甲基吡啶转化为 2-溴-6-甲基吡啶.2-氯吡啶和2-溴吡啶都得到相应的碘化合物.当用原位反应生成的碘三甲基硅烷处理时.尽管 3-和 4-氯吡啶是完全惰性的,但 2,4-二氯吡啶在 2-和 4-位同时进行卤素/卤素交换.卤素置换仅在 2-位与 2,3-二氯吡啶和 2,5-二氯吡啶发生.与作为发生卤素交换的先决条件的 N-三甲基甲硅烷基吡啶鎓盐的中间体一致,2-氟吡啶和 2-氟-6-甲基吡啶和任何 2,6-二卤代吡啶都不发生反应.最后,溴/氯和碘/氯取代也可以用 2-或 4-氯喹啉,1-氯异喹啉,2-氯嘧啶,氯吡嗪和 2,3-二氯喹喔啉作为底物来完成.[在 Scifinder (R) 上]
    DOI:10.1002/1099-0690(200212)2002:24<4181::Aid-Ejoc4181>3.0.Co;2-M

    专利信息


    专利号:US-12150934-B2
    优先权日:2016-11-30
    标 题 :Methods of using substituted pyrazole and pyrazole compounds and for treatment of hyperproliferative diseases
    发明人:SIDDIQUI ARSHAD M; CIBLAT STEPHANE; CONSTANTINEAU-FORGET LEA; GRAND-MAITRE CHANTAL; GUO XIANGYU; SRIVASTAVA SANJAY; SHIPPS GERALD W; COOPER ALAN B; OZA VIBHA; KOSTURA MATTHEW W; LUTHER MICHAEL; LEVINE JEDD
    权利人:BANTAM PHARMACEUTICAL LLC
    摘要:Disclosed are methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for use and uses in medicaments. In certain embodiments, the methods, uses and compounds are provided with reference to compounds of the structural formula (I), in which X1, X2, Z1, Z2, the ring system denoted by “aâ€?, R1, L1, L2, Q, L3, R3, L4, R4, L5, and R5 are as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene.

    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-2012172350-A1
    优先权日:2009-09-11
    标题 :Histamine h3 inverse agonists and antagonists and methods of use thereof
    发明人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN
    权利人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SUNOVION PHARMACEUTICALS INC
    摘要:Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.

    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:WO-9743267-A1
    优先权日:1996-05-11
    标题:Pyrazines
    发明人:HIBBERT FRANK; JONES KEITH; KEENAN MARTINE
    权利人:KING S COLLEGE LONDON; HIBBERT FRANK; JONES KEITH; KEENAN MARTINE
    摘要:There are provided novel pyrazines and a method of making them by reacting 5-halo substituted pyrazines with an arylboronic acid, the novel pyrazines can be used in the synthesis of coelenterazine.

    专利号:US-6849631-B2
    优先权日:2000-12-08
    标 题 :Semicarbazides and their uses
    发明人:CARINI DAVID J
    权利人:BRISTOL MYERS SQUIBB PHARMA CO
    摘要:The present invention relates to the synthesis of a new class of indeno [1,2-c]pyrazol-4-ones of formula (I): n n nthat are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G.n n This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.

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    合成参考文献


    摘要:Sato, N., Science of Synthesis Knowledge Updates, (2011) 4, 276.
    摘要:Wu, Y.; Wang, Jun; Kwong, F. Y., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 636.
    摘要:Kelly, C. B.; Matsui, J. K.; Phelan, J. P.; Gutiérrez Bonet, Á.; Lang, S. B.; Molander, G. A., Science of Synthesis: Photocatalysis in Organic Synthesis, (2018) 1, 361.
    摘要:Telmesani, R.; Sun, A. C.; Beeler, A. B.; Stephenson, C. R. J., Science of Synthesis: Flow Chemistry in Organic Synthesis, (2018) 1, 133.
    摘要:Primer, D. N.; Molander, G. A., Science of Synthesis, (2019) , 288.
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