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Synthesis of [8-3H]Pentostatin

Starting from 3‐(2‐deoxy‐β‐D‐erythro‐pentofuranosyl)‐6,7‐dihydroimidazo[4,5‐d][1,3]diazepin‐8(3H)‐one (4), the synthesis of both the R‐and S‐isomers of [8‐3H]pentostatin has been achieved. The separation of the desired R‐isomer in Ca. 24% overall chemical yield from the R, S‐mixture was effected by preparative reverse‐phase chromatography utilizing a C18 stationary support. Crystalline product of high specific activity (227 mCi/mmole) was obtained.


Putt, S. R., Hartman, J. D., Showalter, H. D. H., Kepler, J., & Taylor, G. (1981). Synthesis of [8-3H]Pentostatin. Journal of Labelled Compounds and Radiopharmaceuticals, 18(7), 925-931. https://doi.org/10.1002/jlcr.2580180702

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