- Synthesis of some halogen- and nitro-substituted nicotinic acids and their fragmentation under electron impact
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Features of electrophilic and nucleophilic substitution under chlorination and nitration reactions conditions have been investigated for 6-hydroxy- and 6-methyl-substituted derivatives of 3-cyano-4-methyl-2(1H)-pyridones. The polychloro- and nitro-substituted 3-cyano-4-methylpyridines obtained were used as synthons in the synthesis of some polyhalo- and nitro-substituted nicotinic acids and their amides. The fragmentation pathways of the synthesized compounds under electron impact have been studied.
- Dyadyuchenko,Strelkov,Mikhailichenko,Zaplishny
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p. 308 - 314
(2007/10/03)
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- Novel Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase. 2. Tricyclic Pyridobenzoxazepinones and Dibenzoxazepinones
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Dibenzoxazepin-11(10H)-ones (III), pyridobenzoxazepin-6(5H)-ones (IV), and pyridobenzoxazepin-5(6H)-ones (V) were found to inhibit human immunodeficiency virus type 1 reverse transcriptase with IC50 values as 19 nM.A-ring substitution has a profound effect on activity, with appropriate substituents at the positions ortho and para to the lactam nitrogen providing dramatically enhanced potency.Substitution in the C-ring is generally neutral or detrimental to activity.Although a C-ring amino substituent at the position meta to the lactam carbonyl is generally beneficial to activity, it has essentially no effect when the A-ring is optimally substituted.Like the dipyridodiazepinone nevirapine, compounds III-V are specific for HIV-1 RT, exhibiting no inhibitory activity against HIV-2 RT or other virial reverse transcriptase enzymes.
- Klunder, Janice M.,Hargrave, Karl D.,West, MaryAnn,Cullen, Ernest,Pal, Kollol,et al.
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p. 1887 - 1897
(2007/10/02)
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- NUCLEOPHILIC SUBSTITUTION REACTIONS IN 2-CHLOROPYRIDINES AND 2,5-DIOXO-1,2,5,7-TETRAHYDRO-1H-FUROPYRIDINES
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3-Cyano- and 3-carbamoyl-2-chloropyridines react with hydrazine hydrate to form substituted 3-amino-1H-pyrazolopyridines and 3-oxo-2,3-dihydro-1H-pyrazolopyridines.Hydrazine hydrate reacts with 3-carbamoyl-2-chloro-5-oxo-5,7-dihydrofuro3,4-
- Kalme, Z. A.,Roloff, B.,Pelcher, Yu. E.,Popelis, Yu. Yu.,Khagen, F.,Dubur, G. Ya
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p. 1031 - 1035
(2007/10/02)
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