244029-95-6 = 1003-31-2 + 6330-51-4 + 2376485-44-6 + 389056-99-9 + 86-84-0 + 5813-89-8 + 313516-36-8 反应条件:1.1 Solvents: Acetonitrile; 60 Min,Rt 标题:Production Of Amidinyl Radicals Via Uv-Vis-Light Promoted Reduction Of N-Arylthiophene-2-Carboxamidoximes And Application To The Preparation Of Some New N-Arylthiophene-2-Carboxamidines 作者:Mekhemer,Islam M. A.; Et Al 参考文献:Acs Omega 日期:2020 卷标:5(44) 页码:28712-28721
专利号:WO-9837078-A1 优先权日:1997-02-20 标题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS 摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The thiophenes are prepared by reaction of a substrate-bound primary or secondary amine with a thiophosgene equivalent and reaction of the resulting intermediate with an acceptor-substituted acetonitrile in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegler-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:US-7598394-B2 优先权日:2003-11-11 标题 :Process for the synthesis of imidazoles 发明人:DOLBY LLOYD J; ESFANDIARI SHERVIN; GARST MICHAEL E 权利人:ALLERGAN INC 摘要:The present invention provides a process for the preparation of imidazoles by reacting a cyano compound with a silylalkylisocyanide compound. Such imidazoles are useful pharmacologically-active compounds and/or intermediates for the preparation of pharmacologically-active compounds.
专利号:US-7880017-B2 优先权日:2003-11-11 标 题 :Process for the synthesis of imidazoles 发明人:DOLBY LLOYD J; ESFANDIARI SHERVIN; GARST MICHAEL E 权利人:ALLERGAN INC 摘要:The present invention provides a process for the preparation of imidazoles by reacting a cyano compound with a silylalkylisocyanide compound. Such imidazoles are useful pharmacologically-active compounds and/or intermediates for the preparation of pharmacologically-active compounds.
专利号:US-2009111737-A1 优先权日:1999-05-24 标题:Novel antibacterial agents 发明人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES 权利人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES 摘要:This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands hasn a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.
专利号:WO-2020242329-A1 优先权日:2019-05-30 标 题:Diketopyrrolopyrroles having three different substituents as emitters of yellow, orange and red light, and the method of their preparation 发明人:PIECZYKOLAN MICHAÅ ; GRYKO DANIEL 权利人:INST CHEMIII ORGANICZNEJ PAN 摘要:New derivatives of diketopyrrolopyrroles (well-known organic pigments) having three different substituents and a new method of obtaining them have been disclosed. These dyes can be used as highly fluorescent substances with advantageous properties. These compounds can be obtained by the method according to the invention in no more than a four-step synthesis from simple, readily available and cheap substrates.
专利号:US-5211889-A 优先权日:1991-08-01 标 题:Soluble highly reactive form of calcium and reagents thereof 发明人:RIEKE REUBEN D 权利人:UNIV NEBRASKA 摘要:A soluble highly reactive form of calcium, prepared from Ca(II) salts and a reducing agent in ethereal, polyethereal, or hydrocarbon solvents, is presented. This form of calcium can be used in the preparation of organocalcium reagents. The organocalcium reagents resulting from the reaction of the soluble highly reactive calcium with organic compounds containing either halide, cyanide, a 1,3-diene, or a polyunsaturated functionality, are stable, useful reagents for organic synthesis. The organocalcium halide reagents undergo Grignard-type reactions. They also undergo reactions with Cu(I) salts to form organocalcium cuprate reagents. The organocalcium cuprate reagents undergo a variety of cross-coupling reactions. The soluble highly reactive calcium reacts with 1,3-dienes to yield the corresponding 2-butene-1,4-diylcalcium complexes. These bis-organocalcium reagents can undergo dialkylation reactions with α,ω-alkylene dihalides and dichlorosilanes to form the corresponding 3-, 5-, and 6-membered ring derivatives. The soluble highly reactive calcium also reacts with organic dihalides to form mono- or diorganocalcium compounds which can be converted into a wide variety of polymers.
[参考文献]: Ming Yu, Et Al. Synthesis Of 2,2'-Bipyrroles And 2,2'-Thienylpyrroles From Donor-Acceptor Cyclopropanes And 2-Cyanoheteroles. Org Lett. 2004 Mar 18;6(6):1057-9. [参考文献]: Tülay A Atein, Et Al. Understanding Selectivity In The Oxidative Addition Of The Carbon-Sulfur Bonds Of 2-Cyanothiophene To Pt(0). Inorg Chem. 2008 Jun 2;47(11):4596-604.
合成参考文献
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