- Synthetic method of 4-chlorine-2-methylpyrimidine
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The invention discloses a synthetic method of 4-chlorine-2-methylpyrimidine. Step1, 2-methyl-4-hydroxypyrimidine, phosphorus oxychloride and organic alkali are mixed by weight ratio of 1 to 5-10 to 0.3-0.7, chlorination reaction is conducted at 25-100 DEG C for 2-5 hours; and step 2, after reaction is completed, the mixture is cooled, then vacuum concentration is conducted to remove the phosphorusoxychloride, after water is added to quench, extraction is conducted by using an organic solvent, and a product is obtained after drying and concentration. According to the synthetic method of the 4-chlorine-2-methylpyrimidine, the synthetic route is short, synthesis is convenient, the yield is high, the toxicity of the raw materials is low, environmental pollution is reduced, and environment-friendly production is achieved.
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Paragraph 0013-0016
(2019/11/12)
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- ANTIVIRAL AGENT
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The present invention provides an integrase inhibitor. The inventors have have found the following compound of formula (I) possessing an integrase inhibitory activity. (wherein, R C and R D taken together with the neighboring carbon atoms form a ring which may be a condensed ring, Y is hydroxy, mercapto or amino; Z is O, S or NH ; R A is a group shown by (wherein, C ring is N-containing aromatic heterocycle) or the like)
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- PIPERAZINE SUBSTITUTED PYRIMIDINE DERIVATIVES AND PHYSIOLOGICALLY TOLERATED SALTS THEREOF
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Pyrimidine derivatives of the formula I I in which R1, R2, R3, R4 and R5 have the indicated meanings, the salts thereof, and a process for the preparation thereof are described. Because of their sorbitol-accumulating activity, they are suitable as a tool in a pharmacological screening model for aldose reductase inhibitors
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- Reactions of Halogenomethanes in the Vapour Phase. Part 5. The Reactions of Imidazolines, Anils, and 1-Methylimidazole with Chloroform at 550 deg C, and a Comparison with their Liquid-Phase Reactions with Trichloroacetate Ion or Hexachloroacetone and Base
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The vapor-phase reactions of imidazolines and anils with chloroform at 550 deg C are compared with their liquid-phase reactions in the presence of hexachloroacetone and base or upon thermolysis with trichloroacetate ion.In the vapour-phase reactions imidazolines, unlike imidazoles, gave non-chlorinated pyrimidines, and 1-methyl-imidazole gave 2-cyanopyrrole and the four 3-chlorocyanopyridines.
- Busby, Reginald E.,Khan, Mohammad A.,Khan, Mohammad R.,Parrick, John,Shaw, C. J. Granville
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p. 1431 - 1435
(2007/10/02)
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- Reactions of Halogenomethanes in the Vapor Phase. Part 4. The Reactions of Imidazoles with Chloroform at 550 deg C, and a Comparison with their Liquid-phase Reactions with Trichloroacetate Ion or Hexachloroacetone and Base
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1-Unsubstituted imidazoles and chloroform at 550 deg C in a flow system give mainly 5-chloropyrimidines, together with 4-chloropyrimidines and chloropyrazines.The effects of methyl substituents on the ratio of products is considered.The liquid-phase reactions of 2-methyl- and 2,4,5-trimethyl-imidazole under conditions in which dichlorocarbene is said to be formed in basic or neutral conditions were studied, and compared with the gas-phase reactions with chloroform.
- Busby, Reginald E.,Khan, Mohammad A.,Khan, Mohammad R.,Parrick, John,Shaw, C. J. Granville,Iqbal, Mohammad
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p. 1427 - 1430
(2007/10/02)
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