4-硝基甲苯置于tetramethylammonium Hydrogen Sulfate体系中,化学反应 0.25H,以88%的收率获得产物3-碘苯甲酸 参考文献:Tetraalkylammonium Dichloroiodates As Iodinating Agents: Absence Of Activity In Solid Phases And Superelectrophilic Activity In Sulfuric Acid 标题:Tetraalkylammonium Dichloroiodates As Iodinating Agents: Absence Of Activity In Solid Phases And Superelectrophilic Activity In Sulfuric Acid 摘要:与已发表的结果相反,四烷基铵二氯碘酸盐(alk4N+icl2-)在无溶剂条件下不能作为芳烃的碘化试剂.然而,在硫酸溶液中或在与硫酸中的ag2So4存在下,四烷基铵二氯碘酸盐表现出超亲电子特性,并作为非常方便和高效率的碘化试剂用于非活化芳烃. DOI:10.1055/s-2008-1032026
专利号:EP-1641729-B1 优先权日:2003-07-09 标题:Use of functionalized onium salts as a soluble support for organic synthesis 发明人:VAULTIER MICHEL; GMOUH SAID; HASSINE FATIMA 权利人:CENTRE NAT RECH SCIENT; UNIV RENNES 摘要:The invention relates to the use of a onium salt functionalized by at least one organic function, as a soluble support, in the presence of at least one organic solvent, for organic synthesis of a molecule, in a homogenous phase, by at least one transformation of said organic function. The onium salt enables the synthesized molecule to be released. The onium salt is present in liquid or solid form at room temperature and corresponds to formula A1+, X1-, wherein A1+ represents a cation and X1- represents an anion.
专利号:WO-2013117440-A1 优先权日:2012-02-09 标 题 :Synthesis of water-soluble phosphine oxides by pd/c-catalyzed p-c coupling in water 发明人:RANOCCHIARI MARCO; RUMMELT STEPHAN; VAN BOKHOVEN JEROEN A 权利人:SCHERRER INST PAUL 摘要:Cross-coupling between diphenylphosphine oxide and halogenated benzoic acids catalyzed by Pd/C in water is a green, simple and fast protocol to obtain water-soluble tertiary phosphine oxides without the addition of ligands and additives. Low reaction times, microwave irradiation, and high substrate scope make this method general and excellent for lab- and large-scale synthesis without the need to use organic solvents for neither reaction nor workup.
专利号:US-10865163-B2 优先权日:2017-12-20 标题:Carbon dioxide as a directing group for C—H functionalization reactions involving Lewis basic amines, alcohols, thiols, and phosphines for the synthesis of compounds 发明人:YOUNG MICHAEL C; KAPOOR MOHIT 权利人:UNIV TOLEDO 摘要:Methods of synthesizing compounds using CO 2 as a directing group for C—H functionalization, and compounds made thereby, are described.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:WO-2011110511-A1 优先权日:2010-03-11 标题:Spect imaging agents of amyloid plaques 发明人:SCHMITT-WILLICH HERIBERT; HEINRICH TOBIAS; BROCKSCHNIEDER DAMIAN 权利人:Bayer Pharma AG; SCHMITT-WILLICH HERIBERT; HEINRICH TOBIAS; BROCKSCHNIEDER DAMIAN 摘要:The invention relates to novel iodine -radiolabeled compounds useful for diagnosing Alzheimer's desease, to respective novel precursors for the synthesis of such compounds, and to the process of manufacturing said imaging agent of the following Formula (I), wherein Q is a six membered aromatic ring, either carbocycle or heterocycle with one N- atom, wherein X 1 , X 2 , X 3 , X 4 and X 5 are independently selected from N or C, and wherein zero or one of X 1 ( X 2 , X 3 , X 4 or X 5 is N and the remaining ones are C; A is either Sn(alkyl)3, I, l-123, l-124, l-125, l-131, Br; wherein alkyl comprises methyl, ethyl, propyl, butyl, pentyl and hexyl, Y is C or N; with the proviso that if X 1 ( X 2 , X 3 , X 4 or X 5 has the meaning of N, substitution by A in that position is excluded; or a pharmaceutically acceptable salt thereof.
专利号:US-8697032-B2 优先权日:2003-05-02 标题:Prosthetic groups attached to stannyl polymer in the synthesis of radiopharmaceuticals 发明人:HUNTER DUNCAN; GAGNON M KAREN J 权利人:UNIV WESTERN ONTARIO 摘要:The present invention relates to compositions and methods for preparing radiopharmaceutical compounds in high chemical-purity and isotopic-purity. The present invention provides polymer-bound precursors to radiopharmaceutical compounds that can be converted to radiopharmaceutical compounds in one step. In a preferred embodiment, a radiopharmaceutical precursor is bound to a polymeric support via a prosthetic group comprising an alkenyl-tin bond. The radiopharmaceutical precursor is converted to a radiopharmaceutical compound in one step involving cleavage of the alkenyl-tin bond and incorporation of a radioisotope to form the radiopharmaceutical compound. Importantly, the polymeric support containing the toxic tin by-product can be easily removed from the radiopharmaceutical compound by filtration. The present invention can be used to install a large number of different radioisotopes. In a preferred embodiment, the radioisotope is 211 At, 123 I, or 131 I.
摘要:Zhdankin, V. V., Science of Synthesis Knowledge Updates, (2015) 1, 240. 摘要:Saleh, B. A.; Elliott, M. C., Science of Synthesis Knowledge Updates, (2015) 2, 402. 摘要:Yorimitsu, H.; Oshima, K., Science of Synthesis: Water in Organic Synthesis, (2012) 1, 652. 摘要:Eichman, C. C.; Stambuli, J. P., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 383. 摘要:Petit, C.; Montchamp, J.-L., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 337.