2-噻吩基锂置于dinitrogen Tetraoxide体系中,用 四氢呋喃 作为反应溶剂,以76%的收率获得产物2-硝基噻吩 参考文献:Nitration Of Organolithiums And Grignards With Dinitrogen Tetroxide: Success At Melting Interfaces 标题:Nitration Of Organolithiums And Grignards With Dinitrogen Tetroxide: Success At Melting Interfaces 摘要: DOI:10.1021/ja963658E
专利号:US-6995289-B2 优先权日:2000-08-02 标题 :Process for synthesis of alpha, beta-unsaturated ketones 发明人:PATEL IAN; HOPES PHILIP 权利人:ASTRAZENECA AB 摘要:A method for the synthesis of an α,β-unsaturated ketone useful for making substituted 1,4-dihydropyridines is described by reacting an aldehyde with pyrrolidine and then adding a ketone followed by trifluoroacetic acid at low temperature. The synthesis is used in a process for making substituted 1,4-dihydropyridines wherein a vinylogous amide is prepared by reacting a 1,3-cyclohexanedione with a phenylethylamine. The α,β-unsaturated ketone can be reacted with a vinylogous amide to form a 1,5-diketone which can be converted to a substituted 1,4-dihydropyridine.
专利号:US-2008287407-A1 优先权日:2003-12-10 标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use 发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI 权利人:NITROMED INC 摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.
专利号:US-8012993-B2 优先权日:2006-12-28 标题 :Stable S-nitrosothiols, method of synthesis and use 发明人:MOLINER JOSE REPOLLES; COY FRANCISCO PUBILL; MANCINI MARISABEL MOURELLE; NIETO JUAN CARLOS DEL CASTILLO; LLORENTE LYDIA CABEZA; BONIN JUAN MARTINEZ; SALADRIGAS ANA MODOLELL 权利人:LACER SA 摘要:The present invention relates to stable S-nitrosothiols derivatives of formula (I) n nhaving vasodilating effect and which inhibit the aggregation of the platelets and which therefore are useful for the preparation of medicaments for treatment of NO related diseases. The invention also relates to a process for the synthesis of the compounds of formula (I).
专利号:US-2008280855-A1 优先权日:2005-06-22 标 题 :Process For the Production of Intermediates For the Preparation of Tricyclic Benzimidazoles 发明人:CHIESA MARIA VITTORIA; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; SIMON WOLFGANG-ALEXANDER; POSTIUS STEFAN; KROMER WOLFGANG; ZANOTTI-GEROSA ANTONIO 权利人:NYCOMED GMBH 摘要:The invention relates to a process for the synthesis of compounds of the formula 1-a and compounds of the formula 1-b. n n n n n n n n n n The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Ar have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.
专利号:US-9949970-B2 优先权日:2010-09-14 标题 :Synthesis of new benzothiazole derivatives as potential anti-tubercular agents 发明人:KAMAL AHMED; SHETTI RAJESH VCRNC; SWAPNA PONNAMPALLI; AZEEZA SHAIK; REDDY A MALLA; KHAN INSHAD ALI; ABDULLAH SHEIKH TASDUQ; SHARMA SANDEEP; KALIA NITIN PAL 权利人:COUNCIL SCIENT IND RES 摘要:Disclosed are compounds of general formula A useful as potential anti-tubercular agents. The general formula A is
专利号:US-2009326223-A1 优先权日:2006-07-18 标题 :Synthesis of 2-amino-substituted 4-oxo-4h-chromen-8.yl-trifluoro-methanesulfonic acid esters 发明人:GRIFFIN ROGER JOHN; HARDCASTLE IAN ROBERT; DESAGE-EL MURR MARINE; RODRIGUEZ-ARISTEGUI SONSOLES; GOLDING BERNARD THOMAS 权利人:GRIFFIN ROGER JOHN; HARDCASTLE IAN ROBERT; DESAGE-EL MURR MARINE; RODRIGUEZ-ARISTEGUI SONSOLES; GOLDING BERNARD THOMAS 摘要:A method of synthesising a compound of formula (I): wherein R N1 and R N2 are independently selected from hydrogen, an optionally substituted C 1-7 alkyl group, C 3-20 heterocyclyl group, or C 5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; from a compound of formula (III): comprising the steps of: (a) removing the allyl group from the compound of formula (III) with appropriate reaction conditions to yield a compound of formula (II): and (b) reacting the compound of formula (II) with a triflating agent to yield a compound of formula (I).
参考标题:Palladium-Catalyzed Four-Component Carbonylative Synthesis Of 2,3-Disubstituted Quinazolin-4(3H)-Ones: Convenient Methaqualone Preparation 作者:Jin-Bao Peng,Hui-Qing Geng,Wei Wang,Xinxin Qi,Jun Ying,Xiao-Feng Wu |发布日期:2018.9 摘要:A Palladium-Catalyzed Four-Component Carbonylative Cyclization Reaction For The Synthesis Of 2,3-Disubstituted Quinazolin-4(3H)-Ones Has Been Developed. A Range Of Different 2,3-Disubstituted Quinazolin-4(3H)-One Derivatives Were Prepared In Moderate To Good Yields Employing Simple And Readily Accessible 2-Iodoanilines, Nitro Compounds And Acid Anhydrides As The Synthetic Precursors. Mo(Co)6 Acted
合成参考文献
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