- Preparation method of 2-methyl-5-aminotrifluorotoluene
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The invention provides a preparation method of 2-methyl-5-aminotrifluorotoluene. The method comprises the following steps: reducing 2-trifluoromethylbenzaldehyde, serving as a raw material, with sodium borohydride to obtain 2-trifluoromethyl benzyl alcohol; performing chlorination by sulfoxide chloride to obtain 2-trifluoromethyl benzyl chloride; nitrifying to obtain 2-chloromethyl-5-nitryltrifluorotoluene; lastly, performing hydrogenation reduction to obtain a target product, namely, 2-methyl-5-aminotrifluorotoluene. The method has the advantages of easiness in operation, high product yield, low cost and easiness in industrialization. The chemical formula of the 2-methyl-5-aminotrifluorotoluene is shown in the description.
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- Antihypertensive Activity of 6-Arylpyridopyrimidin-7-amine Derivatives
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A series of 51 6-arylpyridopyrimidin-7-amine derivatives was prepared and evaluated for antihypertensive activity in the conscious spontaneously hypertensive rat.A number of these compounds, notably 6-(2,6-dichlorophenyl)-2-methylpyridopyrimidin-7-amine (36), lowered blood pressure in these rats in a gradual and sustained manner to normotensive levels at oral doses of 10-50 mg/kg.Normalized blood pressure levels could then be maintained by single daily oral doses.The effect of structural variation in the 6-aryl group and in the 2 and 4 positions of the pyridopyrimidine ring on activity is reported and discussed.
- Bennett, Lawrence R.,Blankley, C. John,Fleming, Robert W.,Smith, Ronald D.,Tessman, Deirdre K.
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p. 382 - 389
(2007/10/02)
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