A Phosphoramidite-Based Synthesis of Phosphoramidate Amino Acid Diesters of Antiviral Nucleosides |
| |
| Authors: | Timothy W. Abraham Carston R. Wagner |
| |
| Affiliation: | Department of Medicinal Chemistry, College of Pharmacy , University of Minnesota Minneapolis , Minnesota, 55455, USA |
| |
| Abstract: | Abstract A general synthetic procedure is presented for the preparation of 5′-amino acid phosphoramidates of zidovudine (AZT), 3′-deoxy-2′,3′-didehydrothymidine (D4T), and 3′-fluoro-3′-deoxythymidine (FLT) from their corresponding phosphoramidites. These water soluble amino acid phosphoramidates are more non-polar than the parent nucleoside and exhibit high stability in aqueous media. |
| |
| Keywords: | |
|
|
