Synthesis of Terfenadine Carboxylate |
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| Authors: | Sunil Patel Liladhar Waykole Oljan Repiĉ Kau-Ming Chen |
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| Affiliation: | 1. Technical R &2. D , Chemical R &3. D Sandoz Research Institute, Sandoz Pharmaceuticals Corporation 59 Rt. 10 , East Hanover, New Jersey, 07936, U.S.A. |
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| Abstract: | A synthesis of terfenadine carboxylate, 1, a metabolite of terfenadine 2, is described. In the key step, the sodium salt of 2-(4-bromophenyl)-2-methylpropionic acid, 7, was lithiated via a metal-halogen exchange using t-BuLi and subsequently condensed with 4-[4-(hydroxydiphenylmethylpiperidin-1-yl]butyraldehyde, 5, to afford terfenadine carboxylate, 1. |
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