Processes for the production of fexofenadine

Details Processes for the production of fexofenadine Processes for the production of fexofenadine

2007-02-13

2007-02-13

Chang, Celia (Department: 1625)

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C546S239000

Reexamination Certificate

active

10333974

ABSTRACT:
An improved process for the manufacture of fexofenadine is described in which a compound of formula (F): wherein R2represents COOH, COO—C1-6alkyl or CN; and R3represents hydrogen, mesylate, triflate, tosylate or carboxy-C1-6-alkyl, or a salt thereof is prepared by: (I) reacting a compound of formula (B): wherein R1 represents hydrogen or carboxy-C1-6-alkyl; and R2is a hereinbefore defined, with a copper and/or silver compound in the presence of palladium or a compound thereof to yield a compound of formula (C): wherein R1, and R2are as hereinbefore defined; (II) converting said compound of formula (C) into a compound of formula (E): wherein R2and R3are as hereinbefore defined and R4represents a halogen atom, and (III) reacting said compound of formula (E) with azacyclonol.

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