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.
Azetidine Based Transition State Analogue Inhibitors of N-Ribosyl Hydrolases and Phosphorylases
โ Scribed by Furneaux, Richard H.; Greatrex, Ben; Murkin, Andrew S.; Schramm, Vern L.; Tyler, Peter C.; Evans, Gary B.
- Book ID
- 111677834
- Publisher
- American Chemical Society
- Year
- 2008
- Tongue
- English
- Weight
- 175 KB
- Volume
- 51
- Category
- Article
- ISSN
- 0022-2623
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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