对三氟甲基苯胺置于盐酸,Sodium Nitrite,四羟基二硼体系中,用 甲醇,水 用作溶剂,化学反应 1.5H,以62%的收率获得4-三氟甲基苯硼酸 参考文献:Methanol-Promoted Borylation Of Arylamines: A Simple And Green Synthetic Method To Arylboronic Acids And Arylboronates 标题:Methanol-Promoted Borylation Of Arylamines: A Simple And Green Synthetic Method To Arylboronic Acids And Arylboronates 摘要:A Sandmeyer Borylation Of Arylamines Via A Sn2Ar Pathway Promoted By Methanol With Sodium Nitrite And Hydrochloric Acid As Diazotization Agent Has Been Developed,Which Provide A Simple And Green Synthetic Method To Arylboronic Acids And Arylboronates. Doi:10.1055/s-0033-1339118
专利号:WO-2013057110-A1 优先权日:2011-10-19 标 题:Method for the synthesis of citric acid esters 发明人:ALTENBACH HANS-JOSEF; LANGE KARSTEN; NANDI SUKHENDU; IHIZANE RACHID; JAKOB BERND; SCHNEIDER MANFRED 权利人:BERGISCHE UNI WUPPERTAL; ALTENBACH HANS-JOSEF; LANGE KARSTEN; NANDI SUKHENDU; IHIZANE RACHID; JAKOB BERND; SCHNEIDER MANFRED 摘要:The present invention discloses a targeted synthesis method for the synthesis of asymmetric monoesters and/or symmetrical diesters of citric acid through acidic esterification by using boric acid or a boronic acid as a catalyst. The boric/boronic acid simultaneously acts as a catalyst, as well as a 'protecting group' for the tertiary carboxylic acid, and therefore specifically only the asymmetric monoesters or symmetrical diesters are created.
专利号:WO-2019170204-A1 优先权日:2018-03-05 标 题 :Synthesis of precursors of 2,5-furandicarboxylic acid 发明人:PEDERSEN MARTIN; PEDERSEN CHRISTIAN 权利人:UNIV COPENHAGEN 摘要:The present invention relates to a method for the manufacture of stable FDCA precursors from saccharide derived starting materials. More specific the invention relates to the synthesis of FDCA precursors such as alkyl 5-(hydroxymethyl)furan-2-carboxylates or 5-(hydroxymethyl)furan-2-carboxylic acid in an expedient, practical and environmental benign manner from e.g. D-glucono-δ-lactone. These bio-based monomer building blocks hold great potential in the manufacture of polymer materials.
专利号:US-2025129021-A1 优先权日:2023-09-19 标 题:Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I), Formula (V)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:US-2024309003-A1 优先权日:2021-05-04 标题 :Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN; PANDYA BHAUMIK; KAPLAN ALAN 权利人:VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2â€?). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
专利号:US-9284336-B1 优先权日:2014-08-21 标题 :Synthesis of 4-(pentafluorosulfanyl)benzenediazonium tetrafluoroborate and analogs 发明人:LAALI KENNETH K 权利人:LAALI KENNETH K; UNIV NORTH FLORIDA 摘要:4-(pentafluorosulfanyl)benzenediazonium tetrafluoroborate salt was synthesized and isolated. The pentafluorosulfanyl salt was examined in a wide assortment of reactions to form novel SF 5 -bearing alkenes, alkynes, and biaryl derivatives using Heck-Matsuda, Sonogashira, and Suzuki coupling protocols. Dediazoniation of the salt furnished the corresponding p-SF 5 —C 6 H 4 X, C 6 H 4 OS(O)(CF 3 )â•?NSO 2 CF 3 , and p-SF 5 —C 6 H 4 —NTf 2 derivatives. The azide derivative p-SF 5 —C 6 H 4 N 3 entered into click chemistry with phenylacetylenes to furnish the corresponding triazoles. Various SF 5 -bearing alkenes were synthesized by coupling reactions using a metal catalyst. Fluorodediazoniation selectively furnished the fluoro derivative p-SF 5 —C 6 H 4 F. Homolytic dediazoniation gave the unsymmetrical biaryls, thus demonstrating the broad utility of pentafluorosulfanyl diazonium salts as building blocks of SF5-aromatics that are in high demand in many branches of chemistry including biomedicine and materials chemistry.
专利号:WO-2004058727-A1 优先权日:2002-12-20 标题 :Substituted 3,5-dihydro-4h-imidazol-4-ones for the treatment of obesity 发明人:CHEN YUANWEI; O'CONNOR STEPHEN JAMES; GUNN DAVID; NEWCOM JASON; CHEN JIANQING; YI LIN; ZHANG HAI-JUN; HUNYADI LASZLO MATYAS; NATERO REINA 权利人:BAYER PHARMACEUTICALS CORP; CHEN YUANWEI; O'CONNOR STEPHEN JAMES; GUNN DAVID; NEWCOM JASON; CHEN JIANQING; YI LIN; ZHANG HAI-JUN; HUNYADI LASZLO MATYAS; NATERO REINA 摘要:This invention relates to substituted 3,5-dihydro-4H-imidazol-4-ones compounds which are useful in the treatment of obesity and obesity-related disorders, and as weight-loss and weight-control agents. The invention also provides methods for synthesis of the compounds, pharmaceutical compositions comprising the compounds, and methods of using such compositions for inducing weight loss and treating obesity and obesity-related disorders.
[参考文献]: Ahmed Kamal, Et Al. Synthesis Of Terphenyl Benzimidazoles As Tubulin Polymerization Inhibitors. Eur J Med Chem. 2012 Apr:50:9-17. [参考文献]: Kiyofumi Inamoto, Et Al. Tandem-Type Pd(Ii)-Catalyzed Oxidative Heck Reaction/intramolecular C-H Amidation Sequence: A Novel Route To 4-Aryl-2-Quinolinones. Chem Commun (Camb). 2012 May 7;48(36):4332-4. [参考文献]: M Lakshmi Kantam, Et Al. An Efficient Base-Free N-Arylation Of Imidazoles And Amines With Arylboronic Acids Using Copper-Exchanged Fluorapatite. J Org Chem. 2006 Dec 8;71(25):9522-4. [参考文献]: Navid Dastbaravardeh, Et Al. Ruthenium(0)-Catalyzed Sp3 C-H Bond Arylation Of Benzylic Amines Using Arylboronates. Org Lett. 2012 Apr 6;14(7):1930-3. [参考文献]: S Van Mierloo, Et Al. Combined Experimental-Theoretical Nmr Study On 2,5-Bis(5-Aryl-3-Hexylthiophen-2-Yl)-Thiazolo[5,4-D]Thiazole Derivatives For Printable Electronics. Magn Reson Chem. 2012 May;50(5):379-87.
合成参考文献
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