CAS: 106635-80-7; N4-(2,6-Dimethoxy-4-Methyl-5-(3-(Trifluoromethyl)Phenoxy)Quinolin-8-yl)Pentane-1,4-Diamine

上下游产品

8-[(1-Methyl-4-Nitrobutyl)Amino]-2,6-Dimethoxy-4-Methyl-5-(3-Trifluoromethylphenoxy)Quinoline 622405-66-7
2,6-二甲氧基-4-甲基-5-[3-(三氟甲基)-苯氧基]-8-喹啉胺 8-Amino-2,6-Dimethoxy-4-Methyl-5-<3-(Trifluoromethyl)Phenoxy>Quinoline 106635-86-3
2-[4-[[2,6-二甲氧基-4-甲基-5-[3-(三氟甲基)苯氧基]喹啉-8-基]氨基]戊基]异吲哚-1,3-二酮 2,6-Dimethoxy-4-Methyl-8-<(4-Phthalimido-1-Methylbutyl)Amino>-5-<3-(Trifluoromethyl)Phenoxy>Quinoline 106635-87-4
8-Amino-6-Methoxy-4-Methyl-5-(3-Trifluoromethylphenoxy)Quinoline 82333-41-3
8-氨基-2-氯-6-甲氧基-4-甲基-5-<3-(三氟甲基)苯氧基>喹啉 8-Amino-2-Chloro-6-Methoxy-4-Methyl-5-<3-(Trifluoromethyl)Phenoxy>Quinoline 106635-85-2
6-Methoxy-4-Methyl-8-Phthalimido-5-<3-(Trifluoromethyl)Phenoxy>Quinoline 106635-82-9
2-Chloro-6-Methoxy-4-Methyl-8-Phthalimido-5-<3-(Trifluoromethyl)Phenoxy>Quinoline 106635-84-1
6-Methoxy-4-Methyl-8-Phthalimido-5-<3-(Trifluoromethyl)Phenoxy>Quinoline 1-Oxide 106635-83-0

📜6-Methoxy-4-Methyl-8-Phthalimido-5-<3-(Trifluoromethyl)Phenoxy>Quinoline 1-Oxide置于sodium Hydride,一水合肼,二异丙胺,三氯氧磷体系中,用 乙醇,氯仿,水,N,N-二甲基甲酰胺,乙腈,Paraffin 用作溶剂,化学反应 90.0H,反应生成他非诺喹
参考文献:抗疟药.16.作为候选抗疟药的8-[(4-氨基-1-甲基丁基)氨基]-6-甲氧基-4-甲基-5-[3-(三氟甲基)苯氧基]喹啉的2-取代类似物的合成.
标题:抗疟药.16.作为候选抗疟药的8-[(4-氨基-1-甲基丁基)氨基]-6-甲氧基-4-甲基-5-[3-(三氟甲基)苯氧基]喹啉的2-取代类似物的合成.
摘要:制备了一系列特殊药物8-[(4-氨基-1-甲基丁基)氨基]-6-甲氧基-4-甲基-5-[3-(三氟甲基)苯氧基]喹啉的2-取代类似物(i)并评估其抑制性和预防性抗疟活性.由于该化合物显示出高水平的血液和组织裂殖活性,因此化合物i的类似物的制备受到关注.发现一种类似物8A比母体化合物i具有更高的活性和更低的毒性.此外,制备了实施例8A的三种类似物.尽管三个类似物中的两个显示出显着的抗疟活性,但两者均不如化合物8A.
Doi:10.1021/jm00128A010

专利信息

专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人：GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

专利号:WO-2006046949-A1
优先权日:2004-10-22
标 题 :SYNTHESIS AND ANTIMALARIAL ACTIVITY OF PYRROLO[3,2-f]QUINAZOLINE-1,3- DIAMINE DERIVATIVES
发明人：AI J LIN; JIAN GUAN; QUAN ZHANG; SKILLMAN DONALD R
权利人:WALTER REED ARMY INST OF RES W; AI J LIN; JIAN GUAN; QUAN ZHANG; SKILLMAN DONALD R
摘要:The invention relates to derivatives of pyrroloquinazolinediamine, more specifically derivatives of 7-(substituted)-7H-pyrrolo[3,2-F] quinazoline-1,3-diamines that are non-toxic and are also effective in the treatment of malaria, including P. falciparum and P.vivax strains. The derivatives are certain carbamate derivatives, succinimide derivatives, alkylcarboxamides derivatives and acetamide derivative, phthalimides, alkylamines and all other amide and imide derivatives and their 1-hydroxy analogs,. The derivatives of the present invention are also soluble in common organic solvents to facilitate the purification in a large scale synthesis of the composition.

专利号:US-7253177-B2
优先权日:2004-10-22
标 题:Synthesis and antimalarial activity of pyrrolo[3,2-f]quinazoline-1,3-diamine derivatives
发明人：LIN AI J; GUAN JIAN; ZHANG QUAN; SKILLMAN DONALD R
权利人:US ARMY
摘要:The invention relates to derivatives of pyrroloquinazolinediamine, more specifically derivatives of 7-(substituted)-7H-pyrrolo[3,2-F] quinazoline-1,3-diamines that are non-toxic and are also effective in the treatment of malaria, including P. falciparum and P. vivax strains. The derivatives are certain carbamate derivatives, succinimide derivatives, alkylcarboxamides derivatives and acetamide derivative, phthalimides, alkylamines and all other amide and imide derivatives and their 1-hydroxy analogs. The derivatives of the present invention are also soluble in common organic solvents to facilitate the purification in a large scale synthesis of the composition.

专利号:US-2015158809-A9
优先权日:2013-02-26
标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
发明人：WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
权利人:XENOPORT INC
摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

专利号:WO-2012149093-A1
优先权日:2011-04-26
标 题 :2-guanidino-4-oxo-imidazoline derivatives as antimalarial agents, synthesis and methods of use thereof
发明人：LIN AI J; LIU XIANJUN; KOZAR MICHAEL P; O'NEIL MICHAEL T
权利人:US OF AMERICA AS REPRESENTED BY THE SECRETARY OF ARMY; LIN AI J; LIU XIANJUN; KOZAR MICHAEL P; O'NEIL MICHAEL T
摘要:The present invention relates to new 2-guanidino-4-oxo-imidazoline derivatives (deoxo-IZ), methods of making these compounds, compositions containing the same, and methods of using the same to prevent, treat, or inhibit malaria in a subject.

专利号:US-2007060499-A1
优先权日:2005-09-15
标 题 :Chloroquine combination drugs and methods for their synthesis
发明人：KOSAK KENNETH M
权利人:KOSAK KENNETH M
摘要:This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.