Brigham Young University

Minghong Zhong

Morris J Robins

A process for providing regiospecific and highly stereoselective synthesis of 9-&#x3b2; anomeric purine nucleoside analogs is described. The introduction of the sugar moiety on to 6-(azolyl)-substituted purine bases is performed so that highly stereoselective formation of the &#x3b2; anomers of only the 9 position regioisomers of the purine nucleoside analogs (either D or L enantiomers) is obtained. This regiospecific and stereoselective introduction of the sugar moiety allows the synthesis of nucleoside analogs, and in particular 2'-deoxy, 3&#x2032;-deoxy, 2&#x2032;-deoxy-2&#x2032;-halo-arabino and 2&#x2032;,3&#x2032;-dideoxy-2&#x2032;-halo-threo purine nucleoside analogs, in high yields without formation of the 7-positional regioisomers. Processes for providing novel 6-(azolyl)purines for the regiospecific and highly stereoselective synthesis of 9-&#x3b2; anomeric purine nucleoside analogs are described. The compounds are drugs or intermediates to drugs.

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Minghong Zhong