Modular Synthesis of Constrained Ethyl (cEt) Purine and Pyrimidine Nucleosides
Helen Blade1, Derek Bradley1, Louis Diorazio1
1Pharmaceutical Development, AstraZeneca, Charter Way, Macclesfield SK10 2NA, United Kingdom.
Abstract:
A modular and scalable approach to pyrimidine- and purine-containing constrained ethyl (cEt) nucleosides is demonstrated. Minimizing stereochemical adjustments and protecting group manipulations, diacetone glucose is converted to two representative cEt nucleosides via a functionalized, common intermediate. The retrosynthetic approach to this complex class of drug precursors offers clear benefits over existing routes based on step count and efficiency.
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