CAS: 175278-12-3; 4-Bromo-2-(Trifluoromethoxy)Iodobenzene

1-Methyl-1,4-Diazabicyclo[2.2.2]octan-1-Ium Trifluoromethoxide,5-溴-2-碘苯胺置于pyrilium Tetrafluoroborate,Zirconium(Iv) Oxide体系中,化学反应 1.5H,以73%的收率获得4-溴-2-(三氟甲氧基)碘苯
参考文献:芳香胺到芳基三氟甲基醚的机械化学转化
标题:芳香胺到芳基三氟甲基醚的机械化学转化
摘要:在有机合成和药物化学中对三氟甲氧基的兴趣日益增加,这引发了对适用于天然产物和高度功能化化合物的新的,选择性的,通用的和更快的方法的需求,这些方法适用于"命中率"活动的后期阶段.应用 Pyrylium Tetrafluoroborate,我们开发了一种机械化学方案,以选择性地用 ocf 3官能团取代芳族氨基.我们方法的范围包括 31 个环取代苯胺的例子,包括酰胺和磺胺.以优异的收率获得了预期的 S N Ar 产品.所提出的简洁方法为制药行业开辟了通往新化学空间的途径.
Doi:10.1021/jacs.2C02611

专利信息

专利号:WO-2010096722-A1
优先权日:2009-02-20
标 题 :3-oxo-2, 3-dihydro- [1,2, 4] triazolo [4, 3-a]pyridines as soluble epoxide hydrolase (seh) inhibitors
发明人：FENG JUN; KEUNG WALTER; NOTZ WOLFGANG REINHARD LUDWIG
权利人:TAKEDA PHARMACEUTICAL; FENG JUN; KEUNG WALTER; NOTZ WOLFGANG REINHARD LUDWIG
摘要:Claimed are intermediates in the synthesis of N-Arylmethyl-3-Oxo-2,3-dihydro- [1,2,4]triazolo[4,3-a]pyridine-6-carboxamides as well as a process (A) to arrive at 3-Oxo-2, 3-dihydro-[1,2,4]triazolo[4,3-a]pyridine-6-carboxylic acid. The triazolo[4,3-a]pyridine-6-carboxamides of formula (I) are used as soluble epoxide hydrolase inhibitors (sEH) having therapeutic effect in pathologic conditions such as hypertension, stroke, inflammatory processes, diabetes and a variety of cardiovascular diseases.

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.

专利号:US-8278322-B2
优先权日:2005-08-01
标题 :HCV NS3 protease inhibitors
发明人：HOLLOWAY M KATHARINE; LIVERTON NIGEL J; MCCAULEY JOHN A; RUDD MICHAEL T; VACCA JOSEPH P; LUDMERER STEVEN W; OLSEN DAVID B
权利人:HOLLOWAY M KATHARINE; LIVERTON NIGEL J; MCCAULEY JOHN A; RUDD MICHAEL T; VACCA JOSEPH P; LUDMERER STEVEN W; OLSEN DAVID B; MERCK SHARP & DOHME
摘要:The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

专利号:US-5968938-A
优先权日:1997-06-18
标 题 :Piperazine oxytocin receptor antagonists
发明人：WILLIAMS PETER D; SPARKS MICHELLE A; BELL IAN; GUARE JR JAMES P; FREIDINGER ROGER M
权利人:MERCK & CO INC
摘要:This invention relates to certain novel piperazine 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.