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Synthesis of [14C]-labelled pelrinone

✍ Scribed by D. D. Hicks; J. J. Hangeland

Publisher: John Wiley and Sons
Year: 1987
Tongue: French
Weight: 180 KB
Volume: 24
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.2580240703

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✦ Synopsis

14 CIPelrinone (1,4-d~Qydro-2-methyl-4-0~0-6[ (3-pyridinylrnethy1)amino]-5-pyrimidine-[ C]-carbonitrile hydrochloride; AY-28,768 hydrochloride) , a potent 'notropic agent, was prepared by reacting chloroacetic acid with [ C]sodium cyanide to give the labelled cyanoacetic acid. compound, condensed with acetamidine hydrochloride, coupled with 3-aminomethylpyri~ine, and treated with methanolic hydrochloric acid. Two batches of [ C] firinone were produced, giving a combined overall yield of 15.6% from f C]sodium cyanide (sp. act. 66.2 r 1.5 and 64.2 f 1.9 pCi/mg; 98.8 and 98.0% radiochemical purity, respectively).

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