- A short, facile synthesis of 2-amino-1,5-dihydro-4H-pyrrolo[3,2-d]- pyrimidin-4-one (9-deazaguanine)
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9-Deazaguanine has been synthesized in four steps in an overall isolated yield of 18% from ethyl (ethoxymethylene)cyanoacetate and diethyl aminomalonate.
- Elliott,Montgomery,Walsh
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- ANTIVIRAL AZASUGAR-CONTAINING NUCLEOSIDES
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Disclosed are compounds comprising an azasugar attached to a heterocyclic base, including pharmaceutically acceptable salts thereof, suitable for use in inhibiting viral RNA polymerase activity or viral replication, and treating viral infections. The compounds are characterized, in part, by favorable pharmacokinetics for the active pharmaceutical ingredient, particularly in conjunction with enteral administration, including, in particular, oral administration. Also disclosed are pharmaceutical compositions comprising one or more compounds mentioned above, or pharmaceutically acceptable salts thereof, as well as methods for preparing same. Also provided are methods for inhibiting viral RNA polymerase activity, viral replication, and treating viral infections.
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Page/Page column 103-104
(2014/06/11)
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- COMPOSITIONS AND METHODS FOR INHIBITING VIRAL POLYMERASE
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Provided are compounds of Formula (I) as described herein. Compounds of Formula (I) are useful in methods of inhibiting viral RNA polymerase activity and viral replication. Also provided are pharmaceutical compositions comprising compounds of Formula (I), as well as methods of treating viral infections using compounds of Formula (I).
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Page/Page column 88; 89
(2013/11/05)
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- Development of a practical synthesis of a purine nucleoside phosphorylase inhibitor: BCX-4208
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A practical synthesis of the purine nucleoside phosphorylase (PNP) inhibitor BCX-4208 (1) was accomplished in three telescoped steps. Mannich condensation of the 4-benzyloxy-9-deazahypoxanthine with (3R,4R)-3-hydroxy-4- (hydroxymethyl)pyrrolidine and formaldehyde followed by removal of the protecting group and crystallization furnished the desired product as a hydrochloride salt in 85% overall yield and 99.8% purity. A scalable synthesis of 9-deazahypoxanthine is also reported. 2009 American Chemical Society.
- Kamath, Vivekanand P.,Juarez-Brambila, Jesus J.,Morris, Christopher B.,Winslow, Christopher D.,Morris Jr., Philip E.
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experimental part
p. 928 - 932
(2010/04/22)
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- Carboxy pyrrole, process of preparing and use as precursor
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4-Oxo-4,5-dihydro-3H-pyrrolo[3,2-d] pyrimidine-7-carboxylic acid methyl ester and process for preparing are provided. The 4-oxo-4,5-dihydro-3H-pyrrole[3,2-d] pyrimidine-7-carboxylic acid methyl ester is useful as a precursor for providing 9-deaza-hypoxanthine, a key intermediate for producing certain PNP inhibitors.
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Page/Page column 2
(2008/06/13)
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