Synthesis of tritium- and deuterium-labeled 9-beta-D-arabinofuranosyladenine and the tritium-labeled 5'-monophosphate ester with increased metabolic stability.

Autor: Baker DC, Haskell TH
Jazyk: angličtina
Zdroj: Journal of medicinal chemistry [J Med Chem] 1975 Oct; Vol. 18 (10), pp. 1041-4.
DOI: 10.1021/jm00244a022
Abstrakt: Preparation of both a 5'-deuterium and a 5'-tritium-labeled 9-beta-D-arabinofuranosyladenine (6a and 6b) by reduction of the protected 5'-aldehyde 4 is described. Conversion of 6b to the 5'-tritium-labeled 5'-monophosphate 7b was effected directly with a phosphoryl chloride-formic acid reagent. The product 7b exhibited consistently higher blood levels of nonvolatile tritium than the 2-labeled compound when tested in dogs.
Databáze: MEDLINE