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Premium Synthesis of [ 14 C]ABT‐418, a cholinergic channel activator labeled at two sites on the isoxazole ring
Surber Bruce W.,
Elliott Richard L.,
Kopecka Hana,
Thomas Samuel B.
Publication year1996
Publication title
journal of labelled compounds and radiopharmaceuticals
Resource typeJournals
PublisherJohn Wiley & Sons
Abstract [ 14 C]ABT‐418, (S)‐3‐[ 14 C]methyl‐5‐[N‐methyl‐2‐pyrrolidinyl][4‐ 14 C]isoxazole hydrochloride, was labeled in two positions at maximum specific activity. Starting with 100 mCi of sodium [2‐ 14 C]acetate, 14.6 mCi at 105 mCi/mmol was obtained in 8 steps including the formation of [1,3‐ 14 C]acetone in the pyrolysis of barium [2‐ 14 C]acetate. The key step was the formation of the dianion of [1,3‐ 14 C]acetone oxime and its condensation with L‐proline methyl ester.
Subject(s)acetone , biology , chemistry , cholinergic , hydrochloride , isoxazole , medicinal chemistry , neuroscience , organic chemistry , oxime , ring (chemistry) , sodium acetate , stereochemistry
SCImago Journal Rank0.432

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