CAS: 31462-54-1; 2-Iodopyrimidine

该化合物是一种卤代代环化合物,广泛用作有机合成和制药研究的多用途中间体,其主要优点包括其在相互交织的反应(如铃木-Miyaura和Sonogashira)中具有高度的回动性,使火力环能够高效地发挥作用.碘代金化会增强电益替代,有利于有选择地修改药物发现和材料科学应用.在标准储存条件下的稳定性和与多种反应条件的兼容性进一步有助于其实用性. 2-Iodopyrimidine对于核素类,农用化学品和生物活性分子的合成特别宝贵,使其成为医药和工业化学的关键建筑.

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874676-81-0 183438-24-6 262353-34-4

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CAS号1722-12-9 2-氯嘧啶 | CAS号34671-83-5 2,2'-联嘧啶

合成工艺路线路线简述

    嘧啶置于magnesium Bromide,2,2,6,6-Tetramethylpiperidinylzinc Bromide Lithium Bromide Complex,碘体系中,用 四氢呋喃 用作溶剂,化学反应 12.08H,以97%的收率获得2-碘嘧啶
    参考文献: Chemical Process[fr] Procédé Chimique
    标题: Chemical Process[fr] Procédé Chimique
    摘要:本发明提供了一种生产化合物的方法,该化合物的化学式为(i),其中取代基如权利要求1所定义.本发明还提供了在该方法中使用的中间化合物,以及生产该中间化合物的方法.

    专利信息


    专利号:US-2023399302-A1
    优先权日:2020-10-29
    标题:Process for the preparation of heteroaryl-substituted sulfur(vi) compounds
    发明人:LOPCHUK JUSTIN M; SHULTZ ZACHARY P; SCATTOLIN THOMAS
    权利人:H LEE MOFFITT CANCER CT & RES
    摘要:The present disclosure provides processes for the synthesis of organic compounds, in particular processes for the synthesis of heteroaryl-substituted sulfur(VI) compounds by nucleophilic aromatic substitution.

    专利号:US-10759743-B2
    优先权日:2016-10-24
    标 题 :Pd-catalyzed γ-C(sp3)-H arylation / heteroarylation of free amines
    发明人:YU JIN-QUAN
    权利人:SCRIPPS RESEARCH INST
    摘要:Pd(II)-catalyzed g-G(sp3)-H arylation or heteroarylation of primary amines is realized by using 2-hydroxynicotinaldehyde as a catalytic transient directing group. Importantly, the catalyst and the directing group loading can be lowered to 2% and 4% respectively, thus demonstrating high efficiency of this newly designed transient directing group. Heterocyclic aryl iodides are also compatible with this reaction. Furthermore, swift synthesis of 1,2,3,4-tetrahydronaphthyridine derivatives is accomplished using this reaction.

    专利号:US-9045520-B2
    优先权日:2008-12-23
    标题:Synthesis of purine nucleosides
    发明人:CHUN BYOUNG-KWON; DU JINFA; RACHAKONDA SUGUNA; ROSS BRUCE; SOFIA MICHAEL JOSEPH; PAMULAPATI GANAPATI REDDY; CHANG WONSUK; ZHANG HAI-REN; NAGARATHNAM DHANPALAN
    权利人:CHUN BYOUNG-KWON; DU JINFA; RACHAKONDA SUGUNA; ROSS BRUCE; SOFIA MICHAEL JOSEPH; PAMULAPATI GANAPATI REDDY; CHANG WONSUK; ZHANG HAI-REN; NAGARATHNAM DHANPALAN; GILEAD PHARMASSET LLC
    摘要:A process for preparing phosphoramidate prodrugs or cyclic phosphate prodrugs of nucleoside derivatives, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof.

    专利号:US-2023416243-A1
    优先权日:2020-11-06
    标 题 :Process for Preparing Heterocyclic Methanone Compounds and AZA-Bicyclo Intermediates Thereof
    发明人:GRUGEL CHRISTIAN
    权利人:ACTINOGEN MEDICAL LTD
    摘要:The present disclosure relates to a process for synthesis of heterocyclic methanone compounds, and in particular 3′-substituted, 3-hydroxyl-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1h-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds, and aza-bicyclo intermediates thereof. In particular, the present disclosure also relates to a process for the synthesis of Xanamem. The present disclosure also relates to a process for the synthesis of optionally protected aza-bicyclo intermediate compounds. The present disclosure also relates to 3′-substituted, 3-hydroxyl-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1h-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds and aza-bicyclo intermediate compounds thereof.

    专利号:WO-2024178474-A1
    优先权日:2023-03-02
    标题 :Flow chemistry process for preparing aza-bicyclic heteroaryl compounds
    发明人:WILLIAMS JASON DOUGLAS; PRIESCHL MICHAEL
    权利人:ACTINOGEN MEDICAL LTD
    摘要:The present disclosure relates to a continuous flow process for synthesis of heterocyclic methanone compounds, and in particular 3'-substituted, 3-hydroxyl-(8-aza- bicyclo[3.2.1]oct-8-yl)-[5-(1h-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds, and aza-bicyclo intermediates thereof. In particular, the present disclosure also relates to a continuous flow process that can be utilised toward the synthesis of Xanamem.

    专利号:US-8853228-B2
    优先权日:2007-06-04
    标 题:Heterocyclic analogs of propargyl-linked inhibitors of dihydrofolate reductase
    发明人:ANDERSON AMY C; WRIGHT DENNIS L; FREY KATHLEEN MARY; PAULSEN JANET LEIGH; SCOCCHERA ERIC WILLIAM; VISWANATHAN KISHORE
    权利人:ANDERSON AMY C; WRIGHT DENNIS L; FREY KATHLEEN MARY; PAULSEN JANET LEIGH; SCOCCHERA ERIC WILLIAM; VISWANATHAN KISHORE; UNIV CONNECTICUT
    摘要:The compositions and methods described herein disclose the design, synthesis and testing of compounds that act as inhibitors of DHFR. The basic scaffold of these inhibitors includes a 2,4-diaminopyrimidine ring with a propargyl linker to another substituted aryl, bicyclo or heteroaryl ring. These DHFR inhibitors are potent and selective for many different pathogenic organisms, including the DHFR enzyme from bacteria such as Bacillus anthracis and methicillin-resistant Staphylococcus aureus , fungi such as Candida glabrata, Candida albicans and Cryptococcus neoformans and protozoa such as Cryptosporidium hominis and Toxoplasma gondii . These compounds and other similar compounds are also potent against the mammalian enzyme and may be useful as anti-cancer therapeutics.
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    合成参考文献


    摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 394.
    摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 366.
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