## Abstract Compound 15 – the 2′‐azido analog of the anti‐HIV compound 2′,3′‐didehydro‐2′,3′‐dideoxythymidine – was synthesized. Treatment of 5′‐__O__‐trityl‐β‐D‐ribofuranosylthymine (1) with DAST or MSTF gave the 2,2′‐anhydro derivative 2. The latter and its 3′‐__O__‐benzoate 3 were used for the s
Intracellular metabolism and pharmacokinetics of 5′-hydrogenphosphonate of 3′-azido-2′,3′-dideoxythymidine, a prodrug of 3′-azido-2′,3′-dideoxythymidine
✍ Scribed by Yurii Skoblov; Inna Karpenko; Elena Shirokova; Konstantin Popov; Valerya Andronova; Georgii Galegov; Marina Kukhanova
- Book ID
- 113457125
- Publisher
- Elsevier Science
- Year
- 2004
- Tongue
- English
- Weight
- 155 KB
- Volume
- 63
- Category
- Article
- ISSN
- 0166-3542
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## Abstract The α‐hydroxybenzylphosphonates 1a–1j of the antiviral drug 3′‐azido‐2′,3′‐dideoxythymidine 5 (AZT) as potential lipophilic prodrugs were readily accessible in 49% to 87% yield via a four‐step synthetic pathway introducing the modifications in the aromatic ring system in the last step b
Fatty acyl-glycol phosphate triester conjugates of 3 0 -fluoro-2 0 ,3 0 -dideoxythymidine (FLT) were prepared in three steps from the reaction of diisopropylphoramidous dichloride with fatty acyl-substituted glycols, followed by a coupling reaction with FLT and oxidation with tert-butyl hydroperoxid