- Preparation method for 2-trifluoromethyl-6-aminopurine
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The invention relates to a preparation method for 2-trifluoromethyl-6-aminopurine. The method comprises the following steps: performing a condensation reaction on 4-formyl-5-aminoimidazole and trifluoroacetamide to obtain a compound 1; performing a chlorination reaction on the compound 1 to obtain a compound 2; performing an ammonolysis reaction on the compound 2 and ammonia in an aminolysis reaction solvent; and after the reaction is completed, performing concentration to dryness, adding a solvent, and performing filtration to obtain the 2-trifluoromethyl-6-aminopurine. The preparation methodprovided by the invention has the advantages that raw materials are cheap and easy to obtain, the synthetic steps are simple, the yield is high, the costs are low and the method is suitable for enlarged production.
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Paragraph 0020
(2018/09/08)
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- PHOSPHODIESTERASE 4 INHIBITORS
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PDE4 inhibition is achieved by novel compounds of the Formula (I) wherein R1 and R2 are as defined herein.
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- Synthesis and antirhinovirus activity of 6-(dimethylamino)-2-(trifluoromethyl)-9-(substituted benzyl)-9H-purines
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A series of 6-(dimethylamino)-2-(trifluoromethyl)-9-(substituted benzyl)purines was synthesized and tested for antirhinovirus activity. Most of the compounds were synthesized by alkylation of 6-chloro-2-(trifluoromethyl)-9H-purine with the appropriate benzyl halide followed by displacement of the chloro group with dimethylamine. Alternatively, 6-(dimethylamino)-2-(trifluoromethyl)purine was alkylated with the appropriate benzyl halide. Although several different aryl substituents provided compounds with IC50's = 0.03 μM against rhinovirus serotype 1B, no congener was significantly more active than the parent 2. Twenty-three compounds were tested against 18 other serotypes, but none exhibited a uniform profile of activity.
- Kelley,Linn,Selway
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p. 1757 - 1763
(2007/10/02)
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