邻氯苯磺酰胺置于ammonium Carbonate,Ammonium Hydroxide,Copper(II) Sulfate体系中,化学反应生成 邻氨基苯磺酰胺 参考文献:Hepatitis C Ns5B Polymerase Inhibitors: 4,4-Dialkyl-1-Hydroxy-3-Oxo-3,4-Dihydronaphthalene-3-Yl Benzothiadiazine Derivatives 标题:Hepatitis C Ns5B Polymerase Inhibitors: 4,4-Dialkyl-1-Hydroxy-3-Oxo-3,4-Dihydronaphthalene-3-Yl Benzothiadiazine Derivatives 摘要:4,4-Dialkyl-1-Hydroxy-3-Oxo-3.4-Dihydronaphthalene-3-Yl Benzothiadiazine Derivatives Were Synthesized And Evaluated As Inhibitors Of Genotypes 1A And 1B Hcv Ns5B Polymerase. A Number Of These Compounds Exhibited Potent Activity Against Genotypes 1A And 1B Hcv Polymerase In Both Enzymatic And Cell Culture Activities. A Representative Compound Also Showed Favorable Pharmacokinetics In The Rat. (C) 2008 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Bmcl.2008.06.043
专利信息
专利号:US-2022315528-A1 优先权日:2019-08-21 标题:Inhibitors of phospholipid synthesis and methods of use 发明人:GOUW ARVIN; SCHOW STEVEN R; GREENHOUSE ROBERT J; KLINE TONI; FELSHER DEAN W 权利人:UNIV LELAND STANFORD JUNIOR 摘要:Inhibitors of Glycerol 3-Phosphate Acyltransferase (GPAT) are provided; and methods of use in the treatment of cancer; and treatment of conditions relating to metabolic syndrome, hyperlipidemia, infection and inflammation.
专利号:US-5633400-A 优先权日:1993-01-06 标 题:Process for the preparation of biphenyl derivatives 发明人:WAGNER ADALBERT; BHATNAGAR NEERJA; BUENDIA JEAN; GRIFFOUL CHRISTINE 权利人:HOECHST AG 摘要:The invention relates to a process for the preparation of a compound of the formula (I) ##STR1## in which X is an optionally protected formyl group and n R is a group which is itself inert to the reaction conditions of the synthesis, n which comprises reacting a compound of the formula (II) ##STR2## where X is as defined above, with a substituted phenyl-halogen compound of the formula (III) ##STR3## where the substituent Hal is a halogen group and R is as defined above.
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.
专利号:CN-107033104-B 优先权日:2017-05-16 标题 :A kind of method of asymmetric synthesis of chirality thiazides compounds
专利号:CN-117843549-A 优先权日:2024-01-04 标 题:Method for asymmetric catalytic synthesis of 3,3-disubstituted chiral indole ketone derivatives
专利号:US-11932614-B2 优先权日:2019-12-29 标题 :Method for preparing diazoxide 发明人:QIAO CHUNHUA; XU YIWEN 权利人:UNIV SOOCHOW 摘要:A method for preparing diazoxide includes reacting o-aminobenzenesulfonamide with N-chlorosuccinimide in a chlorine solvent to obtain 2-amino-5-chlorobenzenesulfonamide, mixing the 2-amino-5-chlorobenzenesulfonamide, an imidazole salt and an amide solvent, then heating same for reaction so as to obtain diazoxide; or mixing o-aminobenzenesulfonamide, an imidazole salt and an amide solvent, then heating same for reaction to obtain a compound IV; then reacting the compound IV with N-chlorosuccinimide in a chlorine solvent to obtain diazoxide. The application of imidazole hydrochloride as a catalyst in preparing diazoxide is also disclosed. The present invention avoids the use of highly corrosive and toxic chlorosulfonyl isocyanate, a strong acid (sulfuric acid), and a high reaction temperature (240-250° C.), and the reaction steps are short; the total yield of the two steps is more than 90%, and compared with publicly disclosed preparation methods for diazoxide, the synthesis route overcomes numerous shortcomings, thus being more suitable for industrial production.
[参考文献]: Vullo D, Et Al. Carbonic Anhydrase Inhibitors: Inhibition Of The Tumor-Associated Isozyme Ix With Aromatic And Heterocyclic Sulfonamides. Bioorg Med Chem Lett. 2003 Mar 24;13(6):1005-9. [参考文献]: K Kanamori, Et Al. Nitrogen-15 Nuclear Magnetic Resonance Study Of Benzenesulfonamide And Cyanate Binding To Carbonic Anhydrase. Biochemistry. 1983 May 24;22(11):2658-64. [参考文献]: Robert Rnn, Et Al. Hepatitis C Virus Ns3 Protease Inhibitors Comprising A Novel Aromatic P1 Moiety. Bioorg Med Chem. 2008 Mar 15;16(6):2955-67.
合成参考文献
参考文献:10.1021/jm901855h 摘要:Joseph P, Turtaut F, Ouahrani-Bettache S, Montero JL, Nishimori I, Minakuchi T, Vullo D, Scozzafava A, Köhler S, Winum JY, Supuran CT. Cloning, characterization, and inhibition studies of a beta-carbonic anhydrase from Brucella suis. J Med Chem. 2010 Mar 11;53(5):2277–85. doi: 10.1021/jm901855h. 参考文献:10.1016/j.bmc.2011.06.038 摘要:Nishimori I, Minakuchi T, Vullo D, Scozzafava A, Supuran CT. Inhibition studies of the β-carbonic anhydrases from the bacterial pathogen Salmonella enterica serovar Typhimurium with sulfonamides and sulfamates. Bioorg Med Chem. 2011 Aug 15;19(16):5023–30. doi: 10.1016/j.bmc.2011.06.038.