- One-pot method for preparing chloroquine chloroquine and diiodoquinoline
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The method effectively solves the problems of (1) solving the problem of high isomer ratio in reaction products due to the fact that hydroxyl groups are ortho-alignment positioning groups when no guide groups are first C5 halogenated and C7 iodo, and purification difficulty is also increased. (2) The problems of poor atom economy, harsh reaction conditions, tedious aftertreatment steps and the like in first 66% steps C5 C7 C7 are effectively overcome by the method provided by the invention, and the C5-position halogenated product is 60% effectively overcome by overcoming the defects of poor atom economy, harsh reaction conditions, complicated post-treatment steps and the like in the two methods. The method has the advantages of economy of atoms, simplicity in operation, easiness in amplification and the like.
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- From Surprising Solvothermal Reaction to Uncommon Zinc(II)-Catalyzed Aromatic C-H Activation Reaction for Direct Nitroquinoline Synthesis
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In this work, we first found a surprising solvothermal reaction for direct dinitration of quinoline derivative. To explore the application in direct nitroquinoline synthesis, this reaction was subsequently modified as an equivalent reaction in a Schlenk tube. More significantly, after a constant attempt, nitrated derivative was obtained in optimized condition with a zinc(II) sulfate catalyst, where some substrates with strong electron-withdrawing group were first nitrated by a directly catalyzed condition. This new zinc(II)-catalyzed aromatic C-H activation reaction is the first example of direct dinitration by a single catalyst, which will be a new facile and environmentally friendly strategy to access synthetically useful nitroquinoline derivative.
- Wang, Yazhen,Yu, Feihu,Han, Xiao,Li, Ming,Tong, Yue,Ding, Jie,Hou, Hongwei
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supporting information
p. 5953 - 5958
(2017/05/22)
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- pH-DEPENDENCE OF HYDROLYSIS OF 8-ACETOXYQUINOLINE-5-SULPHONATE IN POLYCATION SOLUTIONS
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The hydrolysis of 8-acetoxyquinoline-5-sulphonate (8-AQS) in aqueous solutions at 30 deg C in the presence of poly(diallyldimethylammonium chloride) (PDDA) and of poly(ethyleneimine) (PEI) has been studied.With both polyelectrolytes a saturation trend of the kinetics has been observed.PDDA was found to reduce the rate of hydrolysis of the substrate only slightly in the pH range 1-8, while it almost triplicates the rate of alkaline hydrolysis.In the presence of PEI the ester undergoes aminolysis and the pH-log(rate) profile appears bell-shaped.The pH dependence of the basicity of the free amino groups and of the fraction of protonated amino groups, involved as binding sites for the substrate, plays an important role.The analysis of the reaction rates showed the remarkable importance of the lower basicity of the leaving group of the substrate when it is associated with both polyions.The influence of the various parameters on the reaction rate has been interpreted by taking into account also the Broensted relationship derived for the aminolysis of 8-AQS by monomeric primary and secondary amines.
- Arcelli, Antonio,Concilio, Carlo
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p. 271 - 278
(2007/10/02)
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