Synthesis and Biological Evaluation of 3-Chloro-4-(D-Ribofuranosyl)-Pyridine and 3-(D-Ribofuranosyl)-2- Pyridone |
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Authors: | M. Belmans I. Vrijens E. L. Esmans J. A. Lepoivre F. C. Alderweireldt L. L. Wotring |
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Affiliation: | 1. Laboratory for Organic Chemistry , University of Antwerp;2. University of Michigan |
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Abstract: | Abstract Condensation of 2-fluoro-3-lithio pyridine and 3-chloro-4-lithio pyridine with 2,4:3,5-di-O-benzylidene-alde-hydo-D-ribose gives the corresponding D-allo- and D-altro-addition products. These were converted into the corresponding mesylates and cyclized to the ribofuranosyl nucleosides with an overall yield of 60–70 %. Both nucleosides did not show any inhibitory effect on L-1210-cells. |
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