CAS: 346-55-4; 4-Chloro-7-Trifluoromethylquinoline

相似化合物

49713-56-6 2568045-34-9 2923492-76-4

上下游产品

7-trifluoromethyl-quinolin-4-ol N-(2-Acetyl-5-trifluoromethyl-phenyl)-formamide Vilsmeier reagent N'-(2-Acetyl-5-trifluoromethyl-phenyl)-N,N-dimethyl-formamidine; hydr°Chloride 4-chloro-7-(trifluoromethyl)-3-quinolinecarboxylic acid 2,6-bis(dimethylaminomethyl)-4-(7'-trifluoromethylquinolin-4'-ylamino)phenol 2,6-bis(N-butyl-N-methylaminomethyl)-4-(7'-trifluoromethylquinolin-4'-ylamino)phenol -4-hydroxyanilino>-7-(trifluoromethyl)quinoline4-3,5-bis(N-pyrrolidinyl)methyl-4-hydroxyanilino-7-(trifluoromethyl)quinoline

📜7-(三氯甲基)-4-羟基喹啉置于三氯氧磷体系中,化学反应 3.0H,反应生成 4-氯-7-三氟甲基喹啉
参考文献:设计,合成和生物学评估4-氨基喹啉-胍基硫脲衍生物作为抗疟剂.
标题:设计,合成和生物学评估4-氨基喹啉-胍基硫脲衍生物作为抗疟剂.
摘要:鸟嘌呤硫脲(gtu)已被确定为重要的抗叶酸抗疟药效基团,而4-氨基喹诺酮类药物具有抗疟活性.在本工作中,使用pf Dhfr酶和血红素单元进行分子对接分析,设计了带有4-氨基喹啉和gtu部分的分子.对接结果表明,必要的相互作用(asp54和ile14)和对接得分(-9.63至-7.36 Kcal / Mmol)与wr99210(-9.89 Kcal / Mol)相当.从这些结果中,选择了九个分子进行合成.在体外,这些合成的化合物的分析揭示出了9个分子的,八显示在0.61-7.55微米的范围抗疟活性pf的d6应变和0.43-8.04μm为pf的w2株.此外,对活性最高的分子进行了分子动力学模拟,以建立这些化合物和参考配体与恶性疟原虫二氢叶酸还原酶(pf Dhfr)的比较结合相互作用.
DOI:10.1016/j.Bioorg.2019.103094

专利信息

专利号:WO-2013138200-A1
优先权日:2012-03-13
标 题 :Green chemistry synthesis of the malaria drug amodiaquine and analogs thereof
发明人：FORTUNAK JOSEPH MARIAN; KULKARNI AMOL ANANT; KING CHRISTOPHER
权利人:UNIV HOWARD
摘要:Methods are provided for a green chemistry one-pot synthesis of amodiaquine and amodiaquine analogs. The methods have a lower environmental impact, lower investment cost, reduced amounts of byproducts and impurities, and a shorter synthesis time, compared to current conventional synthesis methods. The methods reduce the total number of steps in the synthesis from four to five down to two, thereby simplifying production; and allow a reduced number of solvents and reagents to be used in production, thereby reducing the waste generated in the synthesis. The methods can reduce the waste to about 3-5 kilograms of waste generated per kilogram of product produced; and surprisingly improve the overall yield from 60-65% to greater than 90% as compared to the current conventional synthesis methods for amodiaquine and its analogs.

专利号:US-8735586-B2
优先权日:2007-06-26
标 题 :Regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles
发明人：ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR
权利人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR; SANOFI SA
摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct copper catalyzed regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.

专利号:EP-2173747-B1
优先权日:2007-06-26
标 题:A regioselective metal catalyzed synthesis of annelated benzimidazoles and azabenzimidazoles
发明人：ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARE MARC; R KYEN OMAR; URMANN MATHIAS; HALLAND NIS
权利人:SANOFI SA
摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R1; R2; R3; R4; J1; J2; J3; J4 and G have the meanings indicated in the claims. The present invention provides a direct metal, e.g. palladium or copper, catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.

专利号:US-7947701-B2
优先权日:2003-11-14
标题:Dual molecules containing peroxy derivative, the synthesis and therapeutic applications thereof
发明人：CAZELLES JEROME; COSLEDAN FREDERIC; MEUNIER BERNARD; PELLET ALAIN
权利人:SANOFI AVENTIS
摘要:The invention relates to dual molecule compounds containing a peroxide derivative, to processes for the synthesis of such compounds, to pharmaceutical compositions comprising such compounds, and to methods of treatment and prevention of malaria comprising administering such compounds and such pharmaceutical compositions.

专利号:US-2006025327-A1
优先权日:2004-07-30
标 题 :Hybrid molecules QA, wherein Q is an aminoquinoline and a is an antibiotic or a resistance enzyme inhibitor, their synthesis and their uses as antibacterial agent
发明人：SANCHEZ MURIEL; MEUNIER BERNARD
权利人:PALUMED S A & CT NAT DE LA REC
摘要:Aminoquinoline-antibiotic hybrid compounds in the form of hybrid molecules QA, wherein Q is an aminoquinoline and A is an antibiotic or a resistance enzyme inhibitor, their synthesis and their uses as antibacterial agent. This compound is defined by the general formula (I): n nQ-(Y 1 ) p —(U) p′ —(Y 2 ) p″ -A  (I) nin which n Q represents an aminoquinoline, (Y 1 ) p —(U) p′ —(Y 2 ) p″ — is an optional spacer arm and A is an antibiotic, one of its derivatives or precursors, or a resistance enzyme inhibitor. The invention unexpectedly enables the activity of the antibiotic to be improved.

专利号:US-2010261909-A1
优先权日:2007-06-26
标题 :Regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles