- Alpha-substituted pyrimidine-thioalkyl and alkylether compounds as inhibitors of viral reverse transcriptase
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The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula (I) and pyrimidine-thioalkyl and alkylethers of Formula (IA), namely the compounds of Formula (I) where R 4 is selected from the group consisitng of --H or --NR 15 R 16 where R 15 is --H and R 16 is --H, C 1 -C 6 alkyl, NH 2 or R 15 and R 16 taken together with the --N form 1-pyrrolidino, 1-morpholino or 1-piperidino; and R 6 is selected from the group consisting of --H, or halo (preferably --Cl); with the overall proviso that R 4 and R 6 are not both --H. The compounds of Formula (IA) are useful in the treatment of individuals who are HIV positive being inhibitors of viral reverse transcriptase. STR1
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- Electron and Hydrogen Transfer Reductions of Some 2,4-Disubstituted Pyridines
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New synthesis of 2,4-diacetylpyridine 1 was undertaken by Claisen condensation of 2,4-diethoxycarbonylpyridine 2a with ethyl acetate, followed by hydrolysis of the intermediate 3. Reduction of 1 with zinc or its salt in hydrochloric, formic or acetic acids afforded mixtures of the ketocarbinol 4 dicarbinol 5 or diethyl 6 pyridine derivatives. Formation of 6 as the complete reduction product was chemically proved to proceed via 4 and 5. Electrochemical reduction of 2a leads to 2,4-dimethylpyridine 7, and that of 1 gave rise to a mixture of 5 and 6 along with 2,4-diethyl-1,2,5,6-tetrahydropyridine 8 and 2,4-diethylpiperidine 9. Finally, metal hydride reduction of 1 gave 5, and that of diesters 2 or diacid chloride 10 derivatives afforded 2,4-dihydroxymethylpyridine 11.
- Attia, A.,El-Salam, O. I. Abd,Youssef, T. E.
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p. 351 - 362
(2007/10/03)
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