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No-carrier-added Synthesis of 3-[18F]fluoro-1-(2-nitro-1-imidazolyl)-2-propanol. A Potential PET Agent for Detecting Hypoxic but Viable Tissues

No-carrier-added Synthesis of 3-[18F]fluoro-1-(2-nitro-1-imidazolyl)-2-propanol. A Potential PET Agent for Detecting Hypoxic but Viable Tissues

D R Hwang, C S Dence, T A Bonasera, M J Welch

Int J Rad Appl Instrum A. 1989;40(2):117-26.

PMID: 2541102

Abstract:

Four different approaches towards the synthesis of [18F]FMISO have been studied. The first approach was based on the reaction of epoxide 4 and [18F]fluoride. Both specific activity and radiochemical yield (less than 1%) for [18F]FMISO were low. Two new approaches, starting with compounds 8 and 9, have failed to give [18F]FMISO. The fourth approach, based on the reaction of [18F]epifluorohydrin 10, prepared from Tosylate 13 and [18F]KF/Kryptofix 222, has provided a reliable, no-carrier added synthesis of [18F]FMISO. The product was obtained in a radiochemical yield of 7-12% at end-of-synthesis (based on [18F]fluoride) with a specific activity of greater than 400 Ci/mmol and a synthesis time of 1.5 h. Preliminary PET studies suggest that [18F]FMISO may be a promising tracer for delineation of ischemic but viable myocardium.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP503093	Epifluorohydrin		503-09-3	Price

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