1,2-二氟苯置于正丁基锂,羟胺,三氯氧磷体系中,用 四氢呋喃,N,N-二甲基甲酰胺 用作溶剂,化学反应 9.0H,反应生成2,3-二氟苯腈 参考文献: Pyridinone Derivatives As Selective Cytotoxic Agents Against Hiv Infected Cells[fr] Dérivés De Pyridinone Utilisés En Tant Qu'Agents Cytotoxiques Sélectifs Contre Des Cellules Infectées Par Le Vih 标题: Pyridinone Derivatives As Selective Cytotoxic Agents Against Hiv Infected Cells[fr] Dérivés De Pyridinone Utilisés En Tant Qu'Agents Cytotoxiques Sélectifs Contre Des Cellules Infectées Par Le Vih 摘要:本公开涉及公式i的吡啶酮衍生物,其用于选择性杀灭hiv感染的gag-Pol表达细胞,而不对hiv原始细胞产生细胞毒性,并用于治疗hiv感染,或用于治疗,预防或延缓艾滋病或艾滋病相关综合征(arc)的发病或进展.
专利号:WO-0027627-A1 优先权日:1998-11-12 标题 :Aryloxime linkers in the solid-phase synthesis of 3-aminobenzisoxazoles 发明人:WILEY MICHAEL ROBERT; LEPORE SALVATORE DONATO 权利人:LILLY CO ELI; WILEY MICHAEL ROBERT; LEPORE SALVATORE DONATO 摘要:In its first aspect, the invention is directed to a solid support mediated method for the synthesis of diverse polycyclic heterocycles according to general formula (V). A second aspect of the invention is directed to a solid support bound intermediate compound that optionally can be derivatized before a cyclization and displacement procedure provides a product. The intermediate is preferably stable to a wide range of chemical conditions thus allowing, if desired, for the chemical derivatization of the intermediate. A third aspect of the invention is directed to a library of polycyclic heterocycle compounds where said library contains a plurality of diverse library compounds of general formula (V). A fourth aspect of the invention is directed to a method for the synthesis of a library of diverse polycyclic heterocycles by the general method described. A fifth aspect of the invention is directed to an assay kit for the identification of lead compounds of the library described therein.
专利号:WO-9731891-A1 优先权日:1996-03-01 标 题:Process for regioselective substitution of trifluorobenzoate or trifluorobenzonitrile 发明人:LYNCH JOSEPH E; SHI YAO-JUN; WELLS KENNETH M 权利人:MERCK & CO INC; LYNCH JOSEPH E; SHI YAO JUN; WELLS KENNETH M 摘要:The invention provides a process for regioselective substitution of trifluorobenzoate/trifluorobenzonitrile to afford the difluorobenzoate/difluorobenzonitrile in good yields. The resulting difluorobenzoate/difluorobenzonitrile can again be regioselectively substituted with a second nucleophile to give monofluorobenzoate/monofluorobenzonitrile also in good yields. This process is particularly useful for forming key intermediates in the synthesis of oxytocin antagonist compounds.
专利号:US-5777123-A 优先权日:1996-03-01 标题 :Process for regioselective substitution of trifluorobenzoate or trifluorobenzonitrile 发明人:LYNCH JOSEPH E; SHI YAO-JUN; WELLS KENNETH M 权利人:MERCK & CO INC 摘要:The invention provides a process for regioselective substitution of trifluorobenzoate/trifluorobenzonitrile to afford the difluorobenzoate/difluorobenzonitrile in good yields. The resulting difluorobenzoate/difluorobenzonitrile can again be regioselectively substituted with a second nucleophile to give monofluorobenzoate/monofluorobenzonitrile also in good yields. This process is particularly useful for forming key intermediates in the synthesis of oxytocin antagonist compounds.
专利号:US-5087764-A 优先权日:1988-03-10 标 题 :Process for the preparation of 2,3-difluorobenzenes 发明人:REIFFENRATH VOLKER; KRAUSE JOACHIM 权利人:MERCK PATENT GMBH 摘要:1,4-disubstituted 2,3-difluorobenzenes according to formula I are suitable as intermediates for the synthesis of liquid crystalline compounds.
专利号:FR-3094718-A1 优先权日:2019-04-05 标 题:Process for the synthesis of semi-aromatic polyethers
专利号:US-6090805-A 优先权日:1997-06-18 标 题 :Tocolytic oxytocin receptor antagonists 发明人:WILLIAMS PETER D; SPARKS MICHELLE A; BELL IAN; PERLOW DEBRA S; STAUFFER KENNETH; FREIDINGER ROGER M 权利人:MERCK & CO INC 摘要:This invention relates to certain novel benzoxazinone compounds and derivatives thereof, their synthesis, and their use as oxytocin receptor antagonists. One application of these compounds is in the treatment of preterm labor in mammals, especially humans. The ability of the compounds to relax uterine contractions in mammals also makes them useful for treating dysmenorrhea and stopping labor prior to cesarean delivery.
[参考文献]: M Alcolea Palafox, Et Al. Ab Initio Calculations, Ftir And Raman Spectra Of 2,3-Difluorobenzonitrile. Spectrochim Acta A Mol Biomol Spectrosc. 2001 Oct;57(12):2373-89.
合成参考文献
摘要:Ihmels, H., Science of Synthesis Knowledge Updates, (2011) 1, 88. 摘要:Sakya, S. M.; Yang, J., Science of Synthesis Knowledge Updates, (2012) 1, 227.