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Synthesis of [14C]A-62514, a radiolabelled derivative of erythromycin a, via [2-14C]N, N-dimethylethylenediamine

✍ Scribed by Bruce W. Surber; William R. Baker; Louis Seif

Publisher
John Wiley and Sons
Year
1991
Tongue
French
Weight
214 KB
Volume
29
Category
Article
ISSN
0022-2135

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✦ Synopsis

The synthesis of [14C]A-62514, 1 1-deoxy-1 1 -[carboxy(2-dimethylamino-11 -~4C]ethyl)amino]-6-O-methyl-erythromycin A 11,12-(cyclic ester), was performed in five steps. The key intermediate, [2-14C]N,N-dimethylethyl- enediamine, was obtained in 80% yield by reacting Eschenmoser's salt with KI4CN and reducing the resulting [ 1-14C]N,N-dimethylglycinonitriIe with H2 and Raney Ni in methanol and ammonium hydroxide. The final product was obtained 97% radiochemically pure with a specific activity of 39 mCi/mmol. in an overall radiochemical yield of 14%,

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