1256490-44-4Relevant articles and documents
Synthesis of stable isotope labeled analogs of the anti-hepatitis C virus nucleotide prodrugs PSI-7977 and PSI-352938
Chun, Byoung-Kwon,Du, Jinfa,Zhang, Hai-Ren,Chang, Wonsuk,Ross, Bruce S.,Jiang, Ying,Bao, Donghui,Espiritu, Christine L.,Keilman, Meg,Steuer, Holly M. Micolochick,Furman, Phillip A.,Sofia, Michael J.
, p. 886 - 896 (2013/01/15)
In order to support bioanalytical LC/MS method development and plasma sample analysis in preclinical and clinical studies of the anti-hepatitis C-virus nucleotides, PSI-7977 and PSI-352938, the corresponding stable isotope labeled forms were prepared. These labeled compounds were prepared by addition reaction of the freshly prepared Grignard reagent 13CD3MgI to the corresponding 2′-ketone nucleosides followed by fluorination of the resulting carbinol with DAST. As expected, these 2′-C-(trideuterated- 13C-methyl) nucleotide prodrugs showed similar anti-HCV activity to that of the corresponding unlabeled ones. Copyright Pharmasset, Inc..