25063-46-1Relevant academic research and scientific papers
Novel process for synthesizing 4-hydroxy-6-chloroquinoline
-
Paragraph 0011, (2021/06/21)
The invention belongs to the technical field of synthesis of 4-hydroxy-6-chloroquinoline, and particularly relates to a novel process for synthesizing 4-hydroxy-6-chloroquinoline. The process comprises the following steps: S1, cleaning a first reaction container, drying and cooling the container to room temperature, adding parachloroaniline and 5-(methoxymethylene)-2, 2-dimethyl-1, 3-dioxo-4, 6-diketone into an ethanol solution with a certain concentration according to a molar ratio of (0.1-1):(0.1-1), performing slow stirring, and performing reacting for 4-6 hours until the reaction is finished; S2, carrying out suction filtration on the reaction product to obtain 80-95% A; S3, adding a certain amount of diphenyl ether-biphenyl eutectic into a second reaction container, heating the container to 240-260 DEG C, adding the product A, performing stirring,performing reacting for 5-10 minutes, and performing cooling to room temperature; and S4, carrying out suction filtration on a product obtained in the S3 in petroleum ether to obtain 80-90% 4-hydroxy-6-chloroquinoline, and performing drying to obtain a 4-hydroxy-6-chloroquinoline product. According to the method disclosed by the invention, spin-drying is changed into suction filtration, so that a solid product with very high purity can be obtained, and the time is also saved; and in addition, the diphenyl ether-biphenyl eutectic is used as the solvent, so that time, manpower and material resources can be saved.
A Selective and Orally Bioavailable Quinoline-6-Carbonitrile-Based Inhibitor of CDK8/19 Mediator Kinase with Tumor-Enriched Pharmacokinetics
Chen, Mengqian,Cheng, Chen,Chumanevich, Alexander A.,Gorbunova, Svetlana,Li, Jing,McInnes, Campbell,Mindich, Aleksei,Porter, Donald C.,Roninson, Igor B.,Wang, Lili,Zhang, Li
supporting information, (2022/02/16)
Senexins are potent and selective quinazoline inhibitors of CDK8/19 Mediator kinases. To improve their potency and metabolic stability, quinoline-based derivatives were designed through a structure-guided strategy based on the simulated drug–target dockin
Development of novel quinoline-based sulfonamides as selective cancer-associated carbonic anhydrase isoform ix inhibitors
Shaldam, Moataz,Nocentini, Alessio,Elsayed, Zainab M.,Ibrahim, Tamer M.,Salem, Rofaida,El-Domany, Ramadan A.,Capasso, Clemente,Supuran, Claudiu T.,Eldehna, Wagdy M.
, (2021/10/19)
A new series of quinoline-based benzenesulfonamides (QBS) were developed as potential carbonic anhydrase inhibitors (CAIs). The target QBS CAIs is based on the 4-anilinoquinoline scaffold where the primary sulphonamide functionality was grafted at C4 of t
Method for synthesizing organic intermediate compound
-
Paragraph 0048-0050, (2019/12/25)
The invention provides a method for synthesizing an organic intermediate compound. The method comprises the step of synthesizing a compound of formula (I) by taking a compound of formula (II) as a starting material, wherein R is selected from phenyl subst
Direct C-3-alkenylation of quinolones via palladium-catalyzed C-H functionalization
Li, Mingzong,Li, Liangxi,Ge, Haibo
supporting information; experimental part, p. 2445 - 2449 (2010/12/25)
An unprecedented C-3-alkenylation of quinolones was reported through palladium-catalyzed C-H functionalization with 1% catalyst loading. This method provides an efficient route to a variety of new quinolone derivatives.
ANTIMALARIAL COMPOUNDS WITH FLEXIBLE SIDE-CHAINS
-
Page/Page column 8, (2009/04/24)
The present invention relates to novel compounds that are inhibitors of wild type and mutant dihydrofolate reductase (DHFR) of Plasmodium falciparum, which are useful for the treatment of malaria. It also relates to processes of making and using such compounds. The antimalarial compounds of the present invention have low toxicity to a host infected with the malarial parasite, and are potent when administered in pharmaceutical compositions.
Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities
Madrid, Peter B.,Sherrill, John,Liou, Ally P.,Weisman, Jennifer L.,DeRisi, Joseph L.,Guy, R. Kiplin
, p. 1015 - 1018 (2007/10/03)
A simple two-step synthesis method was used to make 51 B-ring-substituted 4-hydroxyquinolines allowing analysis of the effect of ring substitutions on inhibition of growth of chloroquine sensitive and resistant strains of Plasmodium falciparum, the dominant cause of malaria morbidity. Substituted quinoline rings other than the 7-chloroquinoline ring found in chloroquine were found to have significant activity against the drug-resistant strain of P. falciparum W2.
