CAS: 612-62-4; 2-Chloroquinoline

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喹啉置于间氯过氧苯甲酸,三氯氧磷体系中,用 二氯甲烷,N,N-二甲基甲酰胺 作为反应溶剂,化学反应生成 2-氯喹啉
参考文献:作为针对 Tlr2 和 P53 途径的潜在辐射防护分子的新型喹啉衍生物的设计,合成,生物学评估和计算机研究
标题:作为针对 Tlr2 和 P53 途径的潜在辐射防护分子的新型喹啉衍生物的设计,合成,生物学评估和计算机研究
摘要:太空电离辐射,辐射装置或核灾难是对人类健康和公共安全的重大威胁.本文以p53凋亡途径和tlr2通路为靶点,寻找潜在的减轻辐射损伤的新型化合物,设计,合成了一系列新型喹啉衍生物,并评价了它们的生物活性.合成的大多数化合物均表现出显着的辐射防护作用,其中该化合物的性能最好.因此,我们验证了其辐射防护活性并研究了其优异活性的机制.结果表明,该化合物不仅显着提高了小鼠受辐射致死后30天的存活率(80%),而且显着减轻了辐射对小鼠造血系统和肠道组织的损伤.机理研究表明,该化合物作用于p53通路,减少辐射诱导的细胞凋亡,同时刺激tlr2上调辐射防护因子的表达.分子动力学研究表明该化合物能够有效地与tlr2蛋白结合,并进一步揭示了结合机制.总而言之,我们研究的所有结果表明喹啉衍生物是一种有效的辐射防护化合物,具有进一步开发的巨大治疗潜力.
DOI:10.1016/j.Ejmech.2024.116239

专利信息

专利号:US-6777553-B1
优先权日:2003-03-25
标题 :Process for synthesis of bis-(substituted-4-quinolyl) disulphides
发明人：MESHRAM HARSHADAS MITARAM; KOKKU PREMALATHA; AYYAGIRI VENKATA MADHAVI; BEGARI ESHWARAIAH; YADAV JHILLU SINGH
权利人:COUNCIL SCIENT IND RES
摘要:The present invention relates to a process for the synthesis of bis-(substituted-4-quinolyl) disulphides.

专利号:US-2008280855-A1
优先权日:2005-06-22
标 题 :Process For the Production of Intermediates For the Preparation of Tricyclic Benzimidazoles
发明人：CHIESA MARIA VITTORIA; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; SIMON WOLFGANG-ALEXANDER; POSTIUS STEFAN; KROMER WOLFGANG; ZANOTTI-GEROSA ANTONIO
权利人:NYCOMED GMBH
摘要:The invention relates to a process for the synthesis of compounds of the formula 1-a and compounds of the formula 1-b. n n n n n n n n n n The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Ar have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.

专利号:US-5212317-A
优先权日:1990-12-20
标 题:Methods and intermediates for the assymmetric synthesis of camptothecin and camptothecin analogs
发明人：COMINS DANIEL L; BAEVSKY MATTHEW F
权利人:UNIV NORTH CAROLINA STATE
摘要:Processes for making compounds of Formulae XIV, XV, and XVII ##STR1## wherein R 6 is lower alkyl, R 7 is lower alkyl, R is lower alkyl, Y is H, F or Cl, R 8 is a moiety of Formula XVIII ##STR2## wherein n is 1, 2, or 3, R 11 is C 1 -C 4 alkyl and R 12 is the same as R 11 , or R 11 and R 12 together form cyclopentane or cyclohexane, and R 13 is: n (a) phenyl substituted 1 to 5 times with C 3 -C 7 secondary alkyl or C 4 -C 7 tertiary alkyl, or n (b) selected from the group consisting of naphthyl, anthryl, and phenanthryl optionally substituted 1 to 5 times with C 3 -C 7 secondary alkyl or C 4 -C 7 tertiary alkyl groups, n R 10 is C 6 -C 10 alkyl, aryl or alkyl aryl, n and Y is H, F or Cl, n are disclosed. These processes can be used to make optically enhanced and optically pure forms of the compounds, which are useful in the making of camptothecin and analogs thereof.

专利号:US-5258516-A
优先权日:1990-12-20
标题 :Optically pure D,E ring intermediates useful for the synthesis of camptothecin and camptothecin analogs
发明人：COMINS DANIEL L; BAEVSKY MATTHEW F
权利人:NC STATE UNIVERSITY
摘要:Processes for making compounds of Formulae XIV, XV, and XVII ##STR1## wherein R 6 is lower alkyl, R 7 is lower alkyl, R is lower alkyl, Y is H, F or Cl, R 8 is a compound of Formula XVIII ##STR2## wherein n is 1, 2, or 3, R 11 is C 1 -C 4 alkyl and R 12 is the same as R 11 , or R 11 and R 12 together form cyclopentane or cyclohexane, and R 13 is: n (a) phenyl substituted 1 to 5 times with C 3 -C 7 secondary alkyl or C 4 -C 7 ; tertiary alkyl, or n (b) selected from the group consisting of naphthyl, anthryl, and phenanthryl optionally substituted 1 to 5 times with C 3 -C 7 secondary alkyl or C 4 -C 7 tertiary alkyl groups, n R 10 is C 6 -C 10 alkyl, aryl or alkyl aryl, n and Y is H, F or Cl, n are disclosed. These processes can be used to make optically enhanced and optically pure forms of the compounds, which are useful in the making of camptothecin and analogs thereof.

专利号:US-3919155-A
优先权日:1970-12-18
标题:Synthesis of aromatic amines by reaction of aromatic compounds with ammonia
发明人：SQUIRE EDWARD NOONAN
权利人:DU PONT
摘要:An improved process for producing an aromatic amine is provided in which an aromatic compound is reacted with ammonia in the presence of a conditioned nickel/nickel oxide cataloreactant at a temperature of from about 150*C. to about 500*C. and at a pressure of from about 10 to about 1000 atmospheres and in the presence of from 1 mole percent to 250 mole percent of water based on the molar amount of the aromatic compound.

专利号:US-4031106-A
优先权日:1973-12-19
标题:Synthesis of aromatic amines by reaction of aromatic compounds with ammonia
发明人：DELPESCO THOMAS WAYNE
权利人:DU PONT
摘要:An improved process is provided for producing an aromatic amine from ammonia and an aromatic compound which comprises reacting the aromatic compound with ammonia at a temperature of from about 150 DEG C. to about 500 DEG C. and at a pressure of from about 10 to about 1000 atmospheres in the presence of a conditioned nickel/nickel oxide/zirconium oxide cataloreactant containing an oxide of lanthanum, samarium, holmium, europium, erbium, yttrium, praseodymium, neodymium, terbium, ytterbium, dysprosium or a mixture of any of them.