AbstractรSyntheses of the `Immucillins', potent aza-C-nucleoside inhibitors of purine nucleoside phosphorylase are reported as well as those of 5-deoxy-, 5-deoxyยฏuoro-and 2-deoxy-analogues and others having modiยฎed bases.
Synthesis of transition state inhibitors for N-riboside hydrolases and transferases
โ Scribed by Richard H Furneaux; Gerrit Limberg; Peter C Tyler; Vern L Schramm
- Publisher
- Elsevier Science
- Year
- 1997
- Tongue
- French
- Weight
- 752 KB
- Volume
- 53
- Category
- Article
- ISSN
- 0040-4020
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โฆ Synopsis
A number of 1,4--didcoxy-l,4-imino-l-(S)-(substituted phenyl)-D-ribitols bearing aromatic OH, NH2, NO2, CO2H and halogeno moieties, and a 3-pyridyl analogue have been s3aithesized. The key step is die condensation of aryllithium or aryl Grignard reagents with the imine 3; derived from the protected 1,4-dideoxy-1,4-imino-D-ribitol 4.
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Synthesis of (Difluoromethyl)phosphonate Azasugars Designed as Inhibitors for Glycosyl Transferases. -With a view to designing compounds with the title biological activity different azasugars with a CF2 moiety such as (VII) and (VIII) are synthesized. Attempts to improve the yield of (V) are not su