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The synthesis of 1-[(1-methylethyl) amino]-3-{[(4-methyl-thio)-1-naphthalenyl]OXY}-2-propanol hydrochloride-naphthalene-1114C: 4′-methylthiopropranolol

✍ Scribed by D. F. Gransden; G. A. Roth; I. T. Takahashi

Publisher
John Wiley and Sons
Year
1983
Tongue
French
Weight
480 KB
Volume
20
Category
Article
ISSN
0022-2135

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✦ Synopsis

The antihypertensive drug, l-[(l-methylethyl)arnino]-3-

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 l-naphtholl-%.

The overall yield for the synthesis was 3 3 . 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.

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