CAS: 35853-45-3; 2,8-Bis(Trifluoromethyl)-4-Bromoquinoline

相似化合物

35853-48-6 1239460-75-3 260973-10-2

上下游产品

CAS号35853-41-9 2,8-双(三氟甲基)-4-羟基喹啉 | CAS号1031928-53-6 2,8-BIS(TRIFLUO... | CAS号68496-04-8 alpha-2-pyridin... | CAS号57120-54-4 2-[2,8-BIS(TRIF...

2,8-双(三氟甲基)-4-羟基喹啉置于三溴氧磷体系中,用98%的收率获得产物4-溴-2,8-二(三氟甲基)喹啉
参考文献:(+)-抗-和(-)-顺-甲氟喹盐酸盐的不对称合成
标题:(+)-抗-和(-)-顺-甲氟喹盐酸盐的不对称合成
摘要:描述了从一个常见的中间体不对称(er> 99:1)合成(+)-抗-和(-)-顺甲氟喹盐酸盐的方法.sharpless不对称二羟基化反应是该中间体合成中使用的关键不对称转化.它是在可从市售材料中以三个步骤访问的烯烃上进行的,从而使整个合成过程非常简洁.源自无尖锐不对称二羟基化的普通二醇中间体被转化为反式或顺式环氧化物,随后将它们分别转化为(+)-抗-和(-)-顺式-甲氟喹.(+)-的衍生物的x射线晶体学分析抗-和(-)-顺甲氟喹用于躺着休息关于mefloquines的绝对立体化学40年的说法.还提出了使用(+)-抗甲氟喹盐酸盐的正式不对称(er> 99:1)合成方法,该方法使用sharpless不对称环氧化作为关键步骤.
DOI:10.1021/acs.Joc.6B01476

专利信息

专利号:US-6500955-B1
优先权日:2001-02-02
标 题:One pot synthesis of [2,8-Bis (trifluoromethyl)-4-quinolinyl]-2-pyridinylmethanone, a mefloquine intermediate
发明人：CHAWLA HARMANDER PAL SINGH; JOHAR PERMINDER SINGH; MITTAL ALKA; MEENA RAM AVTAR; NEGI VILLENDRA SINGH
权利人:NAT INST OF PHARMACEUTICAL EDU
摘要:The present invention provides a simple single step process for the preparation of [2,8-bis(trifluoromethyl)-4-quinolinyl]-2-pyridinylmethanone, comprising the step of condensing a halo-quinoline with an alpha-picolyl derivatives in the presence of a solvent, a base and a phase transfer catalyst at −10° C. to +90° C.

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:CN-1370777-A
优先权日:2001-02-02
标题:Improved single-reactor synthesis of [2,8-di(trifluoromethyl)-4-quinolyl]-2-pyridyl methyl ketone and methylfluoro quine

专利号:US-2002188129-A1
优先权日:2001-02-02
标题:One pot synthesis of [2, 8-bis (trifluoromethyl)-4- quinolinyl]2-pyridinylmethanone, a mefloquine intermediate