- Selective hydrodechlorination of fluorinated arylamines
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Chlorine-containing polyfluorinated anilines and meta-phenylenediamines undergo selective hydrodechlorination easily upon reduction by zinc in aqueous ammonia. A new approach is thus provided to synthetically valuable, partially fluorinated arylamines based on utilizing polyfluorochloroarenes, which are available as intermediates of perfluoroarene production from perchloroarenes. When chlorine atoms are present in positions both ortho and para to the amino group, para chlorine is initially eliminated. Based on this reaction, a one-pot synthesis of partially fluorinated 4-aminopyridines from 3,5-dichlorotrifluoro- and 3-chlorotetrafluoropyridine has been realized.
- Selivanova, Galina A.,Gurskaya, Larisa Yu.,Pokrovskii, Leonid M.,Kollegov, Vitaliy F.,Shteingarts, Vitaliy D.
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- Preparation method of 4-aminopyridine compound
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The invention discloses a preparation method of a 4-aminopyridine compound. The preparation method comprises the following steps: adding a 4-amino- 3-chloropyridine compound or a 4-amino-3, 5-dichloropyridine compound, potassium phosphate and a catalyst into a solvent, and reacting at 0-10 MPa and 0-100 DEG C for 4-12 hours. According to the preparation method of the 4-aminopyridine compound, therelated raw materials are easy to obtain or self-make, the cost is low, the preparation method is simple, the reaction efficiency is high, the raw material cost is low, and byproducts have economic value; meanwhile, the reaction involved in the invention has good universality and tolerance to functional groups.
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- Novel nucleosides and related processes, pharmaceutical compositions and methods
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The invention provides novel nucleosides and related processes, pharmaceutical compositions, and methods. The novel nucleosides are useful in a wide variety of antiviral, antineoplastic, and antibacterial applications. Preferred embodiments of the instant invention include novel 2 halogen-substituted, 3 halogen-substituted, and 2′,3′dihalogen-substituted analogues of 3-deazaadenosine, and novel 3 halogen-substituted analogues of 3-deazaguanosine. Compounds of the instant invention, including 4-Amino-6-fluoro-1-(β-D-ribofuranosyl)imidazo[4,5-c]pyridine and 6-Amino-7-bromo-1,5-dihydro-1-β-D-ribofuranosylimidazo[4,5-c]pyridin-4-one, have exhibited potent antiviral and anticancer activity in vitro. The compounds are also useful in the concomitant treatment of bacterial infections associated with viral infections such as AIDS.
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Page/Page column 11; Figure 1
(2010/02/07)
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- Synthesis of halogen-substituted 3-deazaadenosine and 3-deazaguanosine analogues as potential antitumor/antiviral agents
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Various 2-halogen-substituted analogues (38, 39, 43 and 44), 3-halogensubstituted analogues (51 and 52), and 2′,3′ -dihalogen- substituted analogues (57-60) of 3-deazaadenosine and 3-halogen-substituted analogues (61 and 62) of 3-deazaguanosine have been synthesized as potential anticancer and/or antiviral agents. Among these compounds, 3-deaza-3-bromoguanosine (62) showed significant cytotoxicity against L1210, P388, CCRF-CEM and B16F10 cell lines in vitro, producing IC50 values of 3, 7, 9 and 7μM, respectively. Several 3-deazaadenosine analogues (38, 51, 57 and 59) showed moderate to weak activity against hepatitis B virus.
- Liu,Luo,Mozdziesz,Lin,Dutschman,Gullen,Cheng,Sartorelli
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p. 1975 - 2000
(2007/10/03)
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- Pyridonecarboxylic acid derivatives or their salts and antibacterial agent comprising the same as the active ingredient
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A pyridonecarboxylic acid derivative represented by the following general formula (1): STR1 [wherein R1 represents hydrogen atom or a carboxyl protective group; R2 represents hydroxyl group, a lower alkoxy group, or a substituted or unsubstituted amino group; R3 represents hydrogen atom or a halogen atom; R4 represents hydrogen atom or a halogen atom; R5 represents a halogen atom or an optionally substituted saturated cyclic amino group; R6 represents hydrogen atom, a halogen atom, nitro group, or an optionally protected amino group; X, Y and Z may be the same or different and respectively represent nitrogen atom, --CH= or --CR7 = (wherein R7 represents a lower alkyl group, a halogen atom, or cyano group) (with the proviso that at least one of X, Y and Z represent the nitrogen atom), and W represents nitrogen atom or --CR8 = (wherein R8 represents hydrogen atom, a halogen atom, or a lower alkyl group)] or its salt, as well as an antibacterial agent containing such compound are provided.
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