Synthesis of terfenadine and derivatives

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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546236, 546237, 546239, C07D21122, C07D21134

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active

061472174

ABSTRACT:
Processes for preparing compounds having the general formula: ##STR1## wherein R.sup.1a is protected carboxy, carboxy, hydroxymethyl, protected hydroxymethyl, or methyl are disclosed. Processes of the invention begin with a starting material of the general formula IV ##STR2## wherein R.sup.1 and R.sup.2 are as defined in the specification.

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Houssin et al. "Piperidine or pyrrolidine analgesic amides . . . " CA 59:1599B, 1964.
Maillard et al. "Anti-inflammatories derivees de l'acide . . . "Chimie Therapeutique 8, 487-494 (1973).
Carr et al. "Synthesis of Terfenadine" Arzneim.-Forsch. 32, 1157-1159 (1982).
Kawai et al. "A Facile Synthesis of an Oxidation Product of Terfenadine" J. Or. Chem. 59, 2620-2622 (1994).
W. Theilheimer Synthetic Methods of Organic Chemistry 26, 192 (1972).

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