专利号:US-7652137-B2 优先权日:2003-03-06 标 题:Synthesis of 5 substituted 7-azaindoles and 7-azaindolines 发明人:GRACZYK PIOTR PAWEL; KHAN AFZAL; BHATIA GURPREET SINGH 权利人:EISAI R&D MAN CO LTD 摘要:The present invention provides a novel substituted azaindoline intermediate of formula (I) and a method for its synthesis. The novel substitued azaindoline intermediate (I) is provided for use in the manufacture of 5-substituted 7-azaindolines and 5-substituted 7-azaindoles.
专利号:US-6465693-B2 优先权日:1998-02-26 标 题 :Metal-catalyzed arylations of hydrazines, hydrazones, and related substrates 发明人:BUCHWALD STEPHEN L; WAGAW SEBLE; GEIS O 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:A method is provided for the transition metal-catalyzed arylation, or vinylation, of hydrazines, hydrazones, and the like. Additionally, the invention provides a conceptually novel strategy, the cornerstone of which is the transition metal-catalyzed arylation or vinylation method, for the synthesis of indoles, carbazoles, and the like. The methods and strategies of the invention may be utilized in standard, parallel, and combinatorial synthetic protocols.
专利号:WO-2023061999-A1 优先权日:2021-10-12 标 题 :Process for preparing a phenolic hydrocarbon 发明人:CORNELLA JOSEP; LE VAILLANT FRANCK 权利人:STUDIENGESELLSCHAFT KOHLE GGMBH 摘要:The present invention discloses a distinct mode of action of a nickel catalyst to forge C-0 bonds to unlock the mild utilization of N2O as O-atom transfer reagent in the synthesis of complex phenols from the corresponding aryl halides.
专利号:WO-0009116-A1 优先权日:1998-08-14 标 题:Grp receptor ligands 发明人:XIANG JIA-NING; KARPINSKI JOSEPH M; CHRISTENSEN SIEGFRIED B IV 权利人:SMITHKLINE BEECHAM CORP; XIANG JIA NING; KARPINSKI JOSEPH M; CHRISTENSEN SIEGFRIED B IV 摘要:Novel GRP receptor antagonists are provided. Methods of using the present compounds to antagonize GRP receptors are also provided. The present invention further involves the synthesis of the present compounds.
专利号:ES-2355726-T3 优先权日:2003-03-06 标题:SYNTHESIS OF 7-AZAINDOLES AND 7-AZAINDOLINAS REPLACED IN POSITION 5.
专利号:WO-2007002173-A1 优先权日:2005-06-22 标 题:Hiv-1 protease inhibitors, and methods of making and using them 发明人:RANA TARIQ M; ALI AKBAR; CAO HONG; SAI KIRAN KUMAR REDDY GA; ANJUM SAIMA GHAFOOR 权利人:UNIV MASSACHUSETTS; RANA TARIQ M; ALI AKBAR; CAO HONG; SAI KIRAN KUMAR REDDY GA; ANJUM SAIMA GHAFOOR 摘要:One aspect of the invention relates to the design, synthesis and biological activity of novel HIV-1 protease inhibitors incorporating N-phenyloxazolidine-5-carboxamides into the (hydroxyethylamino)sulfonamide scaffold as P2 ligands. For example, the present invention relates to inhibitors with variations at the P2 phenyloxazolidine and the P2' phenylsulfonamide moieties. Remarkably, compounds with an (S)-enantiomer of substituted phenyloxazolidines at P2 show highly potent inhibitory activities against wild-type HIV-1 protease. In certain embodiments, the inhibitors of the invention have Ki values in low picomolar (pM) range. In certain embodiments, the inhibitors of the invention were shown to be active against a variety of multi-drug resistant (MDR) HIV-1 proteases, each representing different paradigm of drug resistance.
参考标题:Consequent Construction Of C-C And C-N Bonds Via Palladium-Catalyzed Dual C-H Activation: Synthesis Of Benzo[C]Cinnoline Derivatives 作者:Hongsheng Li,Junhao Zhao,Songjian Yi,Kongzhen Hu,Pengju Feng |发布日期:2021.4.12 摘要:A Highly Efficient Palladium-Catalyzed Cascade Annulation Of Pyrazolones And Aryl Iodides To Access Various Benzo[c]Cinnoline Derivatives Has Been Achieved At 80 °C. A Pyridine-Type Ligand Could Improve The Reaction Efficiency Under Current Reaction Conditions, Giving A Higher Product Yield Up To 94%. This Novel Approach Provided A One-Pot Dual C-H Activation Strategy With Good Functional Group Tolerance
合成参考文献
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