📜2-氨基-3-溴-9-芴酮置于氢氧化钾,一水合肼体系中,化学反应生成2-氨基芴 参考文献:Replacement And Elimination Of Bromine In Bromonitrofluorenones. The Preparation Of 2,3-And 1,2,3-Substituted Fluorenes And Fluorenones 标题:Replacement And Elimination Of Bromine In Bromonitrofluorenones. The Preparation Of 2,3-And 1,2,3-Substituted Fluorenes And Fluorenones 摘要: Doi:10.1021/jo01351A020
专利号:US-5965746-A 优先权日:1997-06-02 标题:Efficient method for the synthesis of N-cyclic maleamic acids and N-cyclic maleimides 发明人:FUJITA SATOSHI; REDDY PAIDI YELLA; TORU TAKESHI 权利人:AISIN SEIKI 摘要:Provided are methods for the synthesis of N-cyclic maleamic acids and N-cyclic maleimide derivatives, as well as N-cyclic maleamic acids and N-cyclic maleimides synthesized thereby. The method for synthesis of an N-cyclic maleamic acid involves reacting an amino group-containing N-cyclic compound with maleic anhydride in acetic acid to obtain an N-cyclic maleamic acid. An N-cyclic maleimide can be formed by adding hexamethyldisilazane to an N-cyclic maleamic acid prepared according to the above-described method, thereby cyclizing a maleamic acid site of the N-cyclic maleamic acid. The described methods allow for the products to be obtained at high yields.
专利号:WO-9931124-A1 优先权日:1997-12-12 标 题:Cholic acid-based scaffolds for multidimensional molecular presentation of peptides 发明人:HOEEG-JENSEN THOMAS 权利人:NOVO NORDISK AS; HOEEG JENSEN THOMAS 摘要:A solid phase method for the synthesis of a plurality of differently substituted cholic acid scaffolds with a wide variety of peptide chain, pseudo-peptide chain or peptoid chain substitutents, as leads or compounds of potential therapeutic interest. The substituted cholic acids are prepared by initial solution synthesis of a scaffold holding amino acids with 3 orthogonal protecting groups. Subsequent solid-phase synthesis provides the build-up of the target molecules, either as discretes or in mixture. The molecules may be screened on the resin or cleaved from the resin and then screened in solution. The method disclosed here provides an easy and fast access to highly diverse compounds, potential peptide mimetics and potential leads for compounds of therapeutic interest. The method is amenable to automatization.
专利号:US-2008221303-A1 优先权日:2004-02-18 标 题:Method for the Preparation of Peptide-Oligonucleotide Conjugates 发明人:KATZHENDLER JEHOSHUA; KLAUZNER YAKIR; BEYLIS IRENA; MIZHIRITSKII MICHAEL; SHPERNAT YAACOV; ASHKENAZI BORIS; FRIDLAND DMITRI 权利人:KATZHENDLER JEHOSHUA; KLAUZNER YAKIR; BEYLIS IRENA; MIZHIRITSKII MICHAEL; SHPERNAT YAACOV; ASHKENAZI BORIS; FRIDLAND DMITRI 摘要:The present invention relates to the synthesis of peptide-oligonucleotide conjugates (POC). More specifically, the invention relates to a novel method for the preparation of peptide-oligonucleotide conjugates, which can be conducted under mild conditions on solid support, can be performed manually or by a synthesizer, can be used to synthesize alternating sequences of peptides and oligonucleotides, and is applicable to the synthesis of a wide variety of peptide-oligonucleotide conjugates constructed from alternate peptide and oligonucleotide blocks.
专利号:US-8034895-B2 优先权日:2004-02-04 标题 :Conjugated thiophenes having conducting properties and synthesis of same 发明人:SKENE WILLIAM G 权利人:UNIV MONTREAL 摘要:The present invention relates to conjugated oligomers and polymers comprising aromatic thiophene cores. The conjugated materials are obtained by simple and efficient condensation of an aryl diamine and an aryl dialdehyde or a bifunctional aryl moiety comprising both an aldehyde and an amine. Condensation of the complementary moieties at temperatures ranging from ambient to refluxing temperatures in various solvents resulted in conjugated oligomers and polymers that can subsequently be cast into thin films. Oligomerization and polymerization can be done under mild conditions with removal of the resulting water bi-product responsible for shifting the equilibrium in favor of the conjugated products. The resulting conjugated compounds can be made conducting with dopants affording electrically conducting materials of either p-type or n-type conductors depending on the dopant selected.
专利号:US-6093825-A 优先权日:1998-05-27 标 题:Methods for preparation of 1,2-dihydroquinolines 发明人:BENDER REINHOLD H W; EDWARDS JAMES P; JONES TODD K 权利人:AMERICAN HOME PROD; LIGAND PHARM INC 摘要:Methods for conversion of anilines to 1,2-dihydroquinolines. 1,2-dihydroquinoliiies are generated from combining an aniline, a silylating agent, and further condensing with a ketone in the presence of a catalyst. In one aspect, the silylation of the aniline may be performed in a one-step synthesis by adding the silylating, agent to the same reaction vessel as the ketone, aniline, and catalyst. In a second aspect, the 1,2-dihydroquinoline is generated in a two-step synthesis where an N-silyl aniline is formed prior to the addition of the ketone and catalyst.
专利号:US-2024207302-A1 优先权日:2021-04-01 标 题 :Antiviral compounds, methods for the manufacturing of compounds, antiviral pharmaceutical composition, use of the compounds and method for the oral treatment of coronavirus infection and related diseases thereof 发明人:CALIXTO JOãO BATISTA; RABI NALLAR JAIME ALBERTO; LOPES E SOUZA THIAGO MORENO 权利人:CALIXTO JOAO BATISTA; RABI NALLAR JAIME ALBERTO; LOPES E SOUZA THIAGO MORENO 摘要:The present invention relates to antiviral compounds selected from cytokinins, their nucleosides and nucleotide analogs, and their prodrugs as inhibitors of viral RNA synthesis, or their salts, solvates, derivatives, or even combinations of aforementioned compounds, for prophylactic treatment, curative (therapeutic) or mitigative coronavirus infection, represented by human and veterinary coronavirus, SARS-COV-2 and MHIV, and for the treatment of individuals potentially exposed to COVID-19. The present invention also comprises the methods for the manufacturing of such compounds, the antiviral pharmaceutical composition containing the compounds of the invention, as well as the use of the compounds, combinations of compounds, and method for the prophylactic, curative (therapeutic) or mitigative treatment of coronavirus infection, represented by coronavirus, in especial SARS-COV-2 and of patients with COVID-19, individual infected with SARS-COV-2 or potentially exposed to this virus. The antiviral activity of the compounds of this invention against SARS-COV-2 was greatly enhanced by inhibiting the 3′-5′-exonuclease. Synergistic results of the compounds according to the present invention were obtained from the combination with repurposed drugs.
1: Ueda O, Kitamura S, Kubo R, Yano Y, Kanzaki Y, Fujimoto T, Tatsumi K, Ohta S. Metabolism of 2-nitrofluorene, 2-aminofluorene and 2-acylaminofluorenes in rat and dog and the role of intestinal bacteria. Xenobiotica. 2001 Jan;31(1):33-49. Review.
合成参考文献
参考文献:10.1038/nsmb.1771 摘要:Rechkoblit O, Kolbanovskiy A, Malinina L, Geacintov NE, Broyde S, Patel DJ. Mechanism of error-free and semitargeted mutagenic bypass of an aromatic amine lesion by Y-family polymerase Dpo4. Nature Structural & Molecular Biology. 2010 Feb 14;17(3):379–88. doi: 10.1038/nsmb.1771.