📜(3,5-Dichloropyridin-1-Ium-1-yl)-Trimethylsilane;Trifluoromethanesulfonate置于fluorine体系中,用 乙腈 用作溶剂,以55%的收率获得n-氟-3,5-二氯吡啶三氟 参考文献:N-Fluoropyridinium Triflate And Its Analogs,The First Stable 1:1 Salts Of Pyridine Nucleus And Halogen Atom 标题:N-Fluoropyridinium Triflate And Its Analogs,The First Stable 1:1 Salts Of Pyridine Nucleus And Halogen Atom 摘要: Doi:10.1016/s0040-4039(00)84772-3
专利信息
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-6262254-B1 优先权日:1997-04-30 标 题 :8-fluoropurine compounds 发明人:BARRIO JORGE R; SATYAMURTHY NAGICHETTIAR; NAMAVARI MOHAMMAD; PHELPS MICHAEL E 权利人:UNIV CALIFORNIA 摘要:An efficient, regiocontrolled approach to the synthesis of 8-fluoropurines by direct fluorination of purines with dilute elemental fluorine, or acetyl hypofluorite, is provided. In a preferred embodiment, a purine compound is dissolved in a polar solvent and reacted with a dilute mixture of F 2 in He or other inert gas.
专利号:WO-0004007-A1 优先权日:1998-07-17 标 题 :Fluorescent dibenzazole derivatives and methods related thereto 发明人:BROWN LAUREN R; XU CHENG 权利人:PROMEGA BIOSCIENCES INC 摘要:Dibenzazole compounds having general structure (I and II), wherein: R1, R2, R3, R4, R5, R6 are independently H or a substituent which aids in solubility of the compound or which provides a linker arm for linking the compound to another moiety; Y is H or a cleavable moiety; X is a hydrogen, halogen, CF3, or SO3H; V and W are oxygen or sulfur; Z is -C=C-, -C C- or an aromatic ring moiety; and n is 0, 1, or 2. When n=0 at least one of R1, R2, R3, R4, and R5 is a substituent which aids in solubility of the compound or which provides a linker arm for linking the compound to another moiety or X is a halogen, CF3 or SO3H. These compounds are highly fluorescent and can be easily detected using a fluorometer. Derivatives in which the Y group is a substituent other than H contain a fluorescence inhibiting chemical moiety that upon removal restores the fluorescence of the compound. Methods for their synthesis and application are provided.
专利号:US-6140051-A 优先权日:1997-07-21 标 题:Fluorescent dibenzazole derivatives and methods related thereto 发明人:BROWN LAUREN R; XU CHENG 权利人:PROMEGA BIOSCIENCES INC 摘要:Dibenzazole compounds having the general structure: wherein; R1, R2, R3, R4, R5, R6 are independently H or a substituent which aids in solubility of the compound or which provides a linker arm for linking the compound to another moiety; Y is H or a cleavable moiety; X is a hydrogen, halogen, CF3, or SO3H; V and W are oxygen or sulfur; Z is -C=C-, -C 3BOND C- or an aromatic ring moiety; and n is 0, 1, or 2. When n=0 at least one of R1, R2, R3, R4, and R5 is a substituent which aids in solubility of the compound or which provides a linker arm for linking the compound to another moiety or X is a halogen, CF3 or SO3H. These compounds are highly fluorescent and can be easily detected using a fluorometer. Derivatives in which the Y group is a substituent other than H contain a fluorescence inhibiting chemical moiety that upon removal restores the fluorescence of the compound. Methods for their synthesis and application are provided.
专利号:WO-9725992-A1 优先权日:1996-01-16 标 题 :Tocolytic oxytocin receptor antagonists 发明人:SPARKS MICHELLE A; FRIEDINGER ROGER M; PERLOW DEBRA S; WILLIAMS PETER D 权利人:MERCK & CO INC; SPARKS MICHELLE A; FRIEDINGER ROGER M; PERLOW DEBRA S; WILLIAMS PETER D 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. 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.