Synthesis of 2′,3′-Dideoxyinosine

Abstract
The synthesis of 2′,3′-dideoxyinosine (ddI, 1) from 2′-deoxyinosine and 2′,3′-dideoxyadenosine (ddA, 2) is described. Chemically, selective benzoylation of the 5′ hydroxyl group of 2′-deoxyinosine is followed by deoxy-genation at the 3′ position via the thioimidazolide 4. De-protection of the resulting 5′-O-benzoyl-2′,3′-dideoxyinosine 5 gave 2′,3′-dideoxyinosine 1. Enzymatically, deamination of ddA 2 with adenosine deaminase also yielded ddI.

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