| Literature DB >> 15158787 |
Dana Hocková1, Antonín Holý, Milena Masojídková, Graciela Andrei, Robert Snoeck, Erik De Clercq, Jan Balzarini.
Abstract
Synthesis of 2,4-diamino-5-cyano-6-[[(diisopropoxyphosphoryl)methoxy]ethoxy]pyrimidine was based on the formation of the pyrimidine ring by cyclization followed by modification of the side chain by alkylation. The 5-cyano group was also transformed to a 5-formyl and 5-hydroxymethyl group by reduction. As a side product an unexpected dimer was formed. Resulting compounds were converted to the free phosphonic acids by treatment with bromotrimethylsilane followed by hydrolysis. The 5-cyano and 5-formyl derivatives showed pronounced antiretroviral activity, comparable to that of the reference drugs adefovir and tenofovir.Entities:
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Year: 2004 PMID： 15158787 DOI： 10.1016/j.bmc.2004.04.002
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641