CAS: 4295-06-1; 4-Chloro-2-Methylquinoline

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50593-69-6 4964-69-6 53342-53-3

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CAS号607-67-0 4-羟基-2-甲基喹啉 | CAS号611-35-8 4-氯喹啉 | CAS号917-54-4 甲基锂 | CAS号497-19-8 纯碱 | CAS号68-12-2 N,N-二甲基甲酰胺 | CAS号5660-24-2 4-羟基-2-甲基喹啉 | CAS号6287-35-0 3-(苯基氨基)-2-丁烯酸乙酯 | CAS号1076-28-4 2-甲基喹啉N-氧化物 | CAS号607-67-0 4-羟基-2-甲基喹啉 | CAS号49612-00-2 4-肼基-2-甲基喹啉 | CAS号19056-26-9 喹地卡明 | CAS号91-63-4 2-甲基喹啉 | CAS号52191-71-6 2-methyl-4-(2-m... | CAS号29196-15-4 2-甲基-4-喹啉甲腈 | CAS号82241-22-3 2-甲基-4-哌嗪喹啉 | CAS号28615-67-0 4-氯喹啉-2-甲醛 | CAS号75896-69-4 4,8-二氯-2-甲基喹啉 | CAS号5660-24-2 4-羟基-2-甲基喹啉

4-羟基-2-甲基喹啉置于三氯氧磷体系中,用 1,4-二氧六环 作为反应溶剂,化学反应 10.0H,反应生成 4-氯喹哪啶
参考文献:新型2-取代-4-氨基喹啉和-喹唑啉作为潜在抗真菌剂的合成和生物学评价
标题:新型2-取代-4-氨基喹啉和-喹唑啉作为潜在抗真菌剂的合成和生物学评价
摘要:为了发现新型抗真菌剂,制备了一系列2-取代-4-氨基喹啉和-喹唑啉,并使用ir,1 H NMR,13 C NMR和hrms光谱技术对其进行了表征.评估了它们对四种侵入性真菌的抗真菌活性,结果显示一些目标化合物表现出中等至极好的抑制效力.最有希望的化合物iii 11,Iii 14,Iii 15和iii 23表现出强效和广谱的抗真菌活性,Mic 值为 4-32 μg/ml.机理研究表明,化合物iii 11 (N,2-Di-P-Tolylquinolin-4-Amine Hydrochloride) 不通过破坏真菌膜发挥抗真菌效力,这与许多传统的膜活性抗真菌药物有很大不同.同时,Iii 11还表现出诱导抗药性的可能性低,并且在小鼠血浆中具有优异的稳定性.此外,还讨论了一些有趣的结构-活性关系(sar).这些结果表明,一些 4-氨基喹啉可作为进一步发现抗真菌药物的新候选药物.
DOI:10.1016/j.Bmcl.2022.128877

专利信息

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-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

专利号:US-2007060558-A1
优先权日:2004-07-30
标 题 :Hybrid molecules QA where Q is an aminoquinoline and A is an antibiotic residue, the synthesis and uses thereof as antibacterial agents
发明人：SANCHEZ MURIEL; MEUNIER BERNARD
权利人:CENTRE NAT RECH SCIENT
摘要:The invention concerns an aminoquinoline-antibiotic hybrid compound of general formula (I): Q—(Y 1 ) p —(U) p —(Y 2 ) p -A: wherein Q represents an aminoquinoline, (Y 1 ) p (U) p —(Y 2 ) p″ is an optional spacer and A is an antibiotic residue. The invention enables the antibiotic residue activity to be unexpectedly enhanced.

专利号:WO-2009000413-A1
优先权日:2007-06-26
标题:A regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles