D. Gransden, G. Roth, I. Takahashi
Sep 1, 1983
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Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
The antihypertensive drug, 1-[(1-methylethyl)amino]-3-{[(4-methylthio)-1-naphthalenyl ]oxy} -2-propanol hydrochloride has been labeled with carbon-14 in the 1-position of the naphthalene. A total of 18.76 mCi was prepared in five steps starting with 1-naphthol-1-14C. The overall yield for the synthesis was 33.6% following five recrystallizations of the free base. The radiochemical purity of the hydrochloride product was 98.0% by high pressure liquid chromatography (HPLC)/liquid scintillation counting (LSC). The specific activity of the product was found to be 11.68 ∓ 0.45 mCi/mmole. Structural confirmation was done by infrared spectroscopy.