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.
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