专利号:US-9126995-B2 优先权日:2011-11-08 标题:Method for catalytic asymmetric synthesis of optically active isoxazoline compound and optically active isoxazoline compound 发明人:TOYAMA KEN-ICHI; MORIYAMA YUJI; MATOBA KAZUTAKA; YAOSAKA MANABU; IKEDA EITATSU 权利人:NISSAN CHEMICAL IND LTD 摘要:There is provided a method for catalytic asymmetric synthesis of optically active isoxazoline compound and an optically active isoxazoline compound. A method for catalytic asymmetric synthesis of optically active isoxazoline compound of a formula (6) including reacting an α,β-unsaturated carbonyl compound of a formula (1) and a hydroxylamine in a solvent in the presence of a base by adding a chiral phase transfer catalyst. An optically active isoxazoline compound of a formula (13) that can be synthesized by the method.
专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:US-7173059-B2 优先权日:2003-05-08 标题:Intermediates useful in the synthesis of HIV-protease inhibitors and methods for preparing the same 发明人:ALBIZATI KIM FRANCIS; BABU SRINIVASAN 权利人:AGOURON PHARMA 摘要:Optically active 3-amino-butene and 1,2-dihydroxy-3-amino-butane intermediate compounds, useful in the synthesis of HIV-protease inhibitors and methods of preparing these intermediate compounds are disclosed.
专利号:US-6700001-B2 优先权日:2001-10-05 标 题:Process for stereoselective synthesis of 2-hydroxymethyl chromans 发明人:GROSS JONATHAN L; STACK GARY P 权利人:WYETH CORP 摘要:A process for the stereoselective synthesis of 2-hydroxymethyl-chromans of formula (II) is providedwhere R, R<1>, R<2 >and R<3 >are as defined herein. The compound of formula (II) is prepared using an optically active benzene compound of formula (I)where R<0 >is as defined herein. The 2-hydroxymethyl-chroman compounds of formula (II) are useful as intermediates for preparing a variety of medicinal agents.
专利号:US-5434152-A 优先权日:1993-11-08 标题:Asymmetric synthesis of (S)-(-)-6-chloro-4- cyclopropyl-3,4-dihydro-4-[(2-pyridyl)ethynyl]-2(1H)-quinazolinone 发明人:HUFFMAN MARK A; YASUDA NOBUYOSHI; DECAMP ANN E; GRABOWSKI EDWARD J J 权利人:MERCK & CO INC 摘要:An asymmetric synthesis of (S)-(-)-6-chloro-4-cyclopropyl-3,4-dihydro-4-[(2-pyridyl)ethynyl]-2(1H)-quinazolinone comprises the chiral addition of 2-pyridylacetylide to N 1 -protected 6-chloro-4-cyclopropyl-2-quinazolinone followed by removal of the protecting group.
专利号:US-9505733-B2 优先权日:2011-11-18 标题:Single step enantioselective process for the preparation of 3-substituted chiral phthalides 发明人:REDDY REKULA SANTOSH; NAGA CHITHANYA KIRAN INDUKURU; ARUMUGAM SUDALAI 权利人:COUNCIL SCIENT IND RES 摘要:The present invention discloses single step, highly enantioselective catalytic oxidative cyclization process for the synthesis of 3-substituted chiral phthalides. In particular, the invention discloses asymmetric synthesis of chiral phthalides via synergetic nitrile accelerated oxidative cyclization of o-cyano substituted aryl alkenes in high yield and enantiomeric excess (ee) in short reaction time. Also, disclosed herein is “one-potâ€? asymmetric synthesis of biologically important natural compounds having 3-substituted chiral phthalide structural framework in the molecule.
[参考文献]: Chimienti M, Et, Al. Comparison Of The Effectiveness Of Dihydroquinidine And Quinidine On Ventricular Ectopy After Acute And Chronic Administration. Cardiovasc Drugs Ther. 1988 Dec;2(5):679-86. [参考文献]: Hermida Js, Et, Al. Hydroquinidine Therapy In Brugada Syndrome. J Am Coll Cardiol. 2004 May 19;43(10):1853-60. [参考文献]: Mazzanti A, Et, Al. Hydroquinidine Prevents Life-Threatening Arrhythmic Events In Patients With Short Qt Syndrome. J Am Coll Cardiol. 2017 Dec 19;70(24):3010-3015. [参考文献]: Chen Zhang, Et Al. Macromolecular Crowding-Assisted Fabrication Of Liquid-Crystalline Imprinted Polymers. Anal Bioanal Chem. 2015 Apr;407(10):2923-31. [参考文献]: Chuan-Wei Jang, Et Al. A Novel Selection Marker For Efficient Dna Cloning And Recombineering In E. Coli. Plos One. 2013;8(2):E57075.
合成参考文献
摘要:Journal of Pharmacology and Experimental Therapeutics., 84(184), 1945 参考文献:10.1016/s0378-4347(00)81606-0 摘要:Reece PA, Peikert M. Simple and selective high-performance liquid chromatographic method for estimating plasma quinidine levels. Journal of Chromatography B: Biomedical Sciences and Applications. 1980 Feb;181(2):207–17. doi: 10.1016/s0378-4347(00)81606-0. 参考文献:10.1016/j.jacc.2003.12.046 摘要:Hermida J, Denjoy I, Clerc J, Extramiana F, Jarry G, Milliez P, Guicheney P, Di Fusco S, Rey J, Cauchemez B, Leenhardt A. Hydroquinidine therapy in Brugada syndrome. Journal of the American College of Cardiology. 2004 May;43(10):1853–60. doi: 10.1016/j.jacc.2003.12.046. 参考文献:10.1007/s00216-020-02866-4 摘要:Zhang L, Wei Z, He S, Huang Y, Liu Z. Preparation, characterization, and application of soluble liquid crystalline molecularly imprinted polymer in electrochemical sensor. Analytical and Bioanalytical Chemistry. 2020 Aug 12;412(26):7321–32. doi: 10.1007/s00216-020-02866-4.