B. Catalanotti et al., Syntheses of [1-N-15]-2'-deoxyinosine, [4-N-15]-2'-deoxyAICAR, and [1-N-15]-2'-deoxyguanosine, EUR J ORG C, (9), 1999, pp. 2235-2239
A high-yield synthesis of [1-N-15]-2'-deoxyinosine (5), [4-N-15]-2'-deoxy A
ICAR (7), and [1-N-15]-2'-deoxyguanosine (10) from 2'-deoxyinosine (1) usin
g relatively low expensive (NH3)-N-15 as N-15 source is described. The meth
od exploits 2-C reactivity of 2'-deoxyinosine (1) to obtain its N-15-labell
ed counterpart, through [1-N-15]-2'-deoxyinosine (5), and successively, [4-
N-15]-2'-deoxyAICAR (7). [1-N-15]-2'-Deoxyguanosine (10) can be prepared as
well, through an improved cyclization procedure. No protection of sugar hy
droxyl groups is required at any stage.