CAS: 35853-41-9; 2,8-Bis(Trifluoromethyl)-4-Hydroxyquinoline

相似化合物

936352-84-0 535993-30-7 1065092-54-7

上下游产品

CAS号372-31-6 三氟乙酰乙酸乙酯 | CAS号88-17-5 2-氨基三氟甲苯 | CAS号35853-45-3 4-溴-2,8-双(三氟甲基)喹啉 | CAS号35853-55-5 双[2,8-二(三氟甲基)喹啉... | CAS号51773-92-3 盐酸甲氟喹 | CAS号83012-13-9 4-氯-2,8-双(三氟甲基)喹啉 | CAS号1031928-53-6 2,8-BIS(TRIFLUO... | CAS号150785-69-6 4-iodo-2,8-bis(... | CAS号68496-04-8 alpha-2-pyridin... | CAS号83012-12-8 alpha,2-pyridyl... | CAS号57120-54-4 2-[2,8-BIS(TRIF...

三氟乙酰乙酸乙酯,邻氨基三氟甲苯置于polyphosphoric Acid体系中,化学反应 3.0H,以91%的收率获得2,8-双(三氟甲基)-4-羟基喹啉
参考文献:新的杂合三氟甲基喹啉类作为抗疟原虫剂.
标题:新的杂合三氟甲基喹啉类作为抗疟原虫剂.
摘要:疟疾仍然是全球范围内的主要公共卫生问题,是造成高发病率和高死亡率的原因.已经确定了对当前抗疟药的耐药性,并且迫切需要新药.在这项研究中,我们基于甲氟喹((2,8-双(三氟甲基)喹啉-4-基)(哌啶-2-基)甲醇)和氨二喹(4-((7-氯喹啉-4-基)氨基)-2-((二乙基氨基)甲基)苯酚)使用环生物等位取代和官能团的分子杂交.在体外针对恶性疟原虫和在感染伯氏疟原虫的小鼠体内评估了该化合物.所有衍生物均呈现抗-P.恶性疟原虫活性,Ic50值为0.083至33.0 µm.具有最佳抗p的化合物.恶性疟原虫活性为n-(5-甲基-4H-1,2,4-三唑-3-基)-2,8-双(三氟甲基)喹啉-4-胺(12)的ic50为0.083 µm.选择三种活性最高的化合物用于针对伯氏疟原虫感染的小鼠的抗疟活性测试.化合物12在感染后第5天最活跃,可将寄生虫病降低66%,这与其体外活性是一致的.这是一个重要的结果
Doi:10.1016/j.Bmc.2019.01.044

专利信息

专利号:WO-2010144434-A1
优先权日:2009-06-09
标题 :Derivatives of mefloquine and associated methods for making and using
发明人：DOW GEOFFREY S; MILNER ERIN E; WIPF PETER; MO TINGTING
权利人:US OF AMERICA AS REPRESENTED BY THE SECRETARY OF THE ARMY ON BEHALF OF U S; DOW GEOFFREY S; MILNER ERIN E; WIPF PETER; MO TINGTING
摘要:The present invention relates to new mefloquine derivatives and therapeutic compositions comprising one or more mefloquine derivatives. Mefloquine derivatives of the invention have a pentafluorosulfanyl moiety substitution at the 8-position. Certain mefloquine derivatives further include a quinoline methanol moiety substitution at the 4-position. The present invention also relates to new intermediate compounds useful in the synthesis of the mefloquine derivatives, which intermediates also have a pentafluorosulfanyl moiety substitution at the 8-position.

专利号:WO-2012107532-A1
优先权日:2011-02-11
标 题 :4-aminoalcoholquinoline derivatives, enantioselective synthesis methods and the use thereof
发明人：JONET ALEXIA; DASSONVILLE-KLIMPT ALEXANDRA; MULLIE CATHERINE; TAUDON NICOLAS; SONNET PASCAL
权利人:UNIV PICARDIE; JONET ALEXIA; DASSONVILLE-KLIMPT ALEXANDRA; MULLIE CATHERINE; TAUDON NICOLAS; SONNET PASCAL
摘要:The present invention is intended to provide new antimalarial compounds with a strong antimalarial activity as well as antibacterial activity with few neurological side effects and a new enantioselective pathway to mefloquine amino-analogs allowing the access of such compounds. The present invention relates to new 4 -aminoalcohol quinoline derivatives of formula (I), as well as the synthesis methods and the uses of such derivatives. In which Y is one selected from formulae (II) to (III). In which Z is selected from formulae (IV) to (VI), and wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and n are as defined in the claims.

专利号:HU-P0401607-A2
优先权日:2004-08-10
标题 :Synthesis of aminoquinoline derivatives and of their starting materials

专利号:EP-2487157-A1
优先权日:2011-02-11
标题 :Enantioselective synthesis method of 4-aminoalcoholquinoline derivatives and the use