pyrimidinones and phosphoramidic-acid

pyrimidinones has been researched along with phosphoramidic-acid* in 1 studies

Other Studies

1 other study(ies) available for pyrimidinones and phosphoramidic-acid

Article	Year
Facile synthesis of the NNRTI microbicide MC-1220 and synthesis of its phosphoramidate prodrugs. Organic & biomolecular chemistry, 2016, Jan-21, Volume: 14, Issue:3 A facile and novel synthetic route to MC-1220 was achieved by condensation of 4,6-dichloro-N,N-5-trimethylpyrimidin-2-amine (1) with the sodium salt of 2,6-difluorophenylacetonitrile, followed by methylation and strong acidic hydrolysis. The prodrugs of MC-1220 were synthesized by reaction of chlorophosphoramidate derivatives (7a-e) or α-acetobromoglucose with the sodium salt of MC-1220. The stability and anti-HIV-1 activity of phosphoramidate prodrugs turned out to be comparable to those of the parent drug MC-1220. Topics: Amides; Anti-HIV Agents; Cells, Cultured; Dose-Response Relationship, Drug; Fluorobenzenes; HIV-1; Humans; Microbial Sensitivity Tests; Molecular Structure; Phosphoric Acids; Prodrugs; Pyrimidinones; Structure-Activity Relationship	2016

Article

Year

Facile synthesis of the NNRTI microbicide MC-1220 and synthesis of its phosphoramidate prodrugs.

Organic & biomolecular chemistry, 2016, Jan-21, Volume: 14, Issue:3

A facile and novel synthetic route to MC-1220 was achieved by condensation of 4,6-dichloro-N,N-5-trimethylpyrimidin-2-amine (1) with the sodium salt of 2,6-difluorophenylacetonitrile, followed by methylation and strong acidic hydrolysis. The prodrugs of MC-1220 were synthesized by reaction of chlorophosphoramidate derivatives (7a-e) or α-acetobromoglucose with the sodium salt of MC-1220. The stability and anti-HIV-1 activity of phosphoramidate prodrugs turned out to be comparable to those of the parent drug MC-1220.

Topics: Amides; Anti-HIV Agents; Cells, Cultured; Dose-Response Relationship, Drug; Fluorobenzenes; HIV-1; Humans; Microbial Sensitivity Tests; Molecular Structure; Phosphoric Acids; Prodrugs; Pyrimidinones; Structure-Activity Relationship

2016