CAS: 170569-87-6; 4-(5-Phenyl-3-(Trifluoromethyl)-1H-Pyrazol-1-yl)Benzenesulfonamide

上下游产品

1-Phenyl-4,4,4-trifluorobutane-1,3-dione 4-hydrazinobenzene-1-sulfonamide hydr°Chloride 1,1,1-trifluoro-4-phenylbut-3-yn-2-one 4-aminosulfonylphenylhydrazine mavacoxib 4-[5-(4-methoxyphenyl)-3-trifluoromethyl-1H-pyrazol-1-yl]benzenesulfonamide 4-[5-(4-(methyl)phenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulphonamide

📜1,1,1-三氟-4-苯基丁-3-炔-2-酮置于1,8-二氮杂双环[5.4.0]十一碳-7-烯体系中,用 二甲基亚砜 用作溶剂,化学反应 48.0H,反应生成塞来昔布杂质3
参考文献:3-或5-Cf 3-吡唑的选择性,无金属方法:Cf 3-壬酮与肼的溶剂转换反应
标题:3-或5-Cf 3-吡唑的选择性,无金属方法:Cf 3-壬酮与肼的溶剂转换反应
摘要:对三氟乙酰化乙炔与芳基(烷基)肼的反应进行了详细的研究,目的在于区域选择性合成3-或5-三氟甲基化的吡唑.发现反应的区域选择性极大地取决于溶剂性质.高极性质子溶剂(六氟异丙醇)有利于3-三氟甲基吡唑的形成.相反,当反应在极性非质子溶剂(dmso)中进行时,优先观测到它们的5-Cf 3-取代的异构体的形成.或者,3-Cf 3的区域选择性组装取代的吡唑可以通过两步一锅法进行.在酸性催化剂存在下三氟甲基化的炔酮与芳基(烷基)肼的反应导致形成相应的.后者可以通过用碱处理平滑地转化为3-Cf 3-吡唑.该溶剂可切换程序用于制备重要药物,如celebrex和sc-560以及其以克为单位的异构体.讨论了可能的反应机理.
Doi:10.1021/acs.Joc.7B00774

专利信息

专利号:US-2003157061-A1
优先权日:2001-12-05
标 题 :Combinations of a cyclooxygenase-2 selective inhibitor and a TNFalpha antagonist and therapeutic uses therefor
发明人：BENNETT DENNIS A
权利人:PHARMACIA CORP
摘要:A method for the prevention, treatment, or inhibition of pain, inflammation, or inflammation-related disorder and for the prevention, treatment, or inhibition of a cardiovascular disease or disorder in a subject that is in need of such prevention, treatment or inhibition, involves the administration to the subject of a cyclooxygenase-2 selective inhibitor or prodrug thereof and a TNFα antagonist. A method can also involve the treatment, prevention, or inhibition of cancer in a subject in need of such treatment, prevention, or inhibition, by administering to the subject a cyclooxygenase-2 selective inhibitor or prodrug thereof and a TNFα antagonist which is selected from the group consisting of a compound that affects the synthesis of TNFα, a compound that inhibits the binding of TNFα with a receptor specific for TNFα, and a compound that interferes with intracellular signaling triggered by TNFα binding with a receptor. Compositions, pharmaceutical compositions and kits that can be used with the methods are also described.

专利号:US-6150534-A
优先权日:1999-01-14
标题:Synthesis of 4-[5-substituted or unsubstituted phenyl)-3-substituted-1H-pyrazol-1-yl]benzenesulfonamides

专利号:US-6232472-B1
优先权日:1999-01-14
标题:Synthesis of 4-[(5-substituted phenyl)-3-substituted-1H-pyrazol-1-yl]benzenesulfonamide
发明人：O'SHEA PAUL; WANG XIN; TILLYER RICHARD D; CLAS SOPHIE-DOROTHEE; DALTON CHAD
权利人:MERCK FROSST CANADA INC
摘要:This invention encompasses a novel process for synthesizing the compound represented by formula I:These compounds are useful as non-steroidal anti-inflammatory agents.

专利号:US-7041694-B1
优先权日:1997-12-17
标 题 :Cyclooxygenase-2 inhibition
发明人：DANNENBERG ANDREW J
权利人:CORNELL RES FOUNDATION INC
摘要:Selective inhibitors of cyclooxygenase-2 are used to treat liver disease and in combination with anti-viral drugs to treat virus-caused liver disorders. Selective inhibitors of cyclooxygenase-2 which also inhibit the synthesis of cyclooxygenase-2 improve over the efficacy of conventional selective inhibitors of cyclooxygenase-2 in the treatment of inflammatory conditions, Alzheimer's disease and cancer.