Synthesis of terfenadine carboxylate

Article abstract of DOI:10.1080/00397919608004796

A synthesis of terfenadine carboxylate, 1, a metabolite of terfenadine 2, is described. In the key step, the sodium salt of 2-(4-bromo-phenyl)-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.

Full text of DOI:10.1080/00397919608004796

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Synthetic Communications: An
International Journal for Rapid
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Organic Chemistry
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Synthesis of Terfenadine
Carboxylate
a
Sunil Patel a , Liladhar Waykole a , Oljan Repiĉ
&
Kau-Ming Chen a
a Technical R & D, Chemical R & D Sandoz Research
Institute, Sandoz Pharmaceuticals Corporation 59
Rt. 10, East Hanover, New Jersey, 07936, U.S.A.
Published online: 21 Aug 2006.
To cite this article: Sunil Patel , Liladhar Waykole , Oljan Repiĉ & Kau-Ming Chen
(1996): Synthesis of Terfenadine Carboxylate, Synthetic Communications: An
International Journal for Rapid Communication of Synthetic Organic Chemistry, 26:24,
4699-4710
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