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.