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Abstract
Practical large-scale synthesis of anti conformationally constrained acyclic nucleosides has been attained from the coupling of lithiated 2,4-dimethoxy-5,6-dimethylpyrimidine with 1,3-bis(tert-butyldiphenylsilyloxy)-propan-2-one, followed by the sequential reactions of methylthiomethylation, ring cyclization, hydrolysis, and desilylation.
ACKNOWLEDGMENTS
We thank Dr. Leroy B. Townsend for supplying 2,4-dimethoxy-5,6-dimethyl pyrimidine as a gift for starting material for chemical synthesis. This investigation is supported by a research grant from the National Science Council of the Republic of China (No. NSC 88-2314-B-016-046).