CAS: 766-11-0; 5-Bromo-2-Fluoropyridine

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5-溴-2-氯吡啶置于四甲基氟化铵体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应 24.0H,以100%的收率获得产物2-氟-5-溴吡啶
参考文献:室温s N Ar氟化的无水四甲基氟化铵
标题:室温s N Ar氟化的无水四甲基氟化铵
摘要:本文介绍了使用无水四甲基氟化铵(nme 4 F)在室温下对芳基卤化物和硝基芳烃进行s N Ar氟化.该试剂在温和的条件下(通常在室温下)有效地将芳基-X(x = Cl,Br,I,No 2,Otf)转化为芳基-F.该反应的底物包括缺电子的杂芳族化合物(22个实例)和芳烃(5个实例).反应的相对速率随x以及底物的结构而变化.但是,一般而言,带有x = No 2的基材或br反应最快.在所检查的所有情况下,这些反应的产率均与在升高的温度(即,更传统的卤代氟化条件)下使用csf所获得的产率相当或更好.反应还提供了可比较的产量,规模从100 Mg到10 G不等.进行了成本分析,结果表明,使用nme 4 F进行氟化处理通常比使用csf进行氟化处理更具成本效益.
DOI:10.1021/acs.Joc.5B02075

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-2024343691-A1
优先权日:2006-12-28
标题:Compositions for modulating a kinase cascade and methods of use thereof
发明人：HANGAUER JR DAVID G; PATRA DEBASIS; CODY JEREMY A; PALMER GRANT J; ISBESTER PAUL K; SALSBURY JONATHON
权利人:ATNX SPV LLC
摘要:The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl) pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.

专利号:US-2024101516-A1
优先权日:2021-01-20
标 题:Synthesis of polyfluorinated aryl and heteroaryl carboxamides
发明人：KADUSKAR RAHUL; BORATE KAILASKUMAR; ADHAV SUYOG; THIRUNAVUKKARASU SARAVANAN; SHINDE HARISH; GOETZ ROLAND
权利人:BASF SE
摘要:The presently claimed invention relates to a process for the preparation of mono-, di-, tri-, fluoro arylamide or hetroarylamide.

专利号:US-8293739-B2
优先权日:2006-12-28
标题:Process for the preparation of compositions for modulating a kinase cascade and methods of use thereof
发明人：HANGAUER JR DAVID G; COUGHLIN DANIEL; GALE JONATHAN; CODY JEREMY A; PATRA DEBASIS; PALMER GRANT J; ISBESTER PAUL K; SALSBURY JONATHON
权利人:HANGAUER JR DAVID G; COUGHLIN DANIEL; GALE JONATHAN; CODY JEREMY A; PATRA DEBASIS; PALMER GRANT J; ISBESTER PAUL K; SALSBURY JONATHON; KINEX PHARMACEUTICALS LLC
摘要:The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. More specifically, the invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy) phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention.

专利号:US-7884125-B2
优先权日:2008-04-30
标 题:Straightforward entry to 7-azabicyclo[2.2.1]heptane-1-carbonitriles and subsequent synthesis of epibatidine analogues
发明人：STEVENS CHRISTIAN; HEUGEBAERT THOMAS
权利人:UNIV GENT
摘要:The present invention relates to a group of substituted-7-azabicyclo-[2.2.1]heptyl derivatives with biological activity. The present invention also relates to synthetic methods for producing said substituted-7-azabicyclo-[2.2.1]heptyl derivatives. The present invention also relates to certain intermediates for producing such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as a synthetic method for producing such intermediates. The present invention also relates to pharmaceutical compositions comprising such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as their use as medicaments for the treatment of diseases mediated by a Nicotinic Acetylcholine Receptor or a receptor being a member of the Neurotransmitter-gated Ion Channel Superfamily, such as pain, Alzheimer's disease, Parkinson's disease, schizophrenia, epilepsy and nicotine addiction.

专利号:US-9242998-B2
优先权日:2013-02-07
标题 :Tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C
发明人：HE SHUWEN; DAI XING; PALANI ANANDAN; NARGUND RAVI; LAI ZHONG; ZORN NICOLAS; XIAO DONG; DANG QUN; MCCOMAS CASEY C; LI PENG; PENG XUANJIA; SOLL RICHARD
权利人:HE SHUWEN; DAI XING; PALANI ANANDAN; NARGUND RAVI; LAI ZHONG; ZORN NICOLAS; XIAO DONG; DANG QUN; MCCOMAS CASEY C; LI PENG; PENG XUANJIA; SOLL RICHARD; MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.