Processes for the production of fexofenadine
AssigneeTexcontor Establissement
InventorFederico Junquera Milla
Life of this patent
Estimating the term…
Abstract
An improved process for the manufacture of fexofenadine is described in which a compound of formula (F): wherein R2 represents COOH, COO—C1-6 alkyl or CN; and R3 represents 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 R2 is 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 R2 are as hereinbefore defined; (II) converting said compound of formula (C) into a compound of formula (E): wherein R2 and R3 are as hereinbefore defined and R4 represents a halogen atom, and (III) reacting said compound of formula (E) with azacyclonol.
Claims17
A process for the preparation of a compound of formula (C)
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- (wherein R1 represents hydrogen or carboxy-C6-1-alkyl;
- and
- R2 represents COOH, COO—C1-6 alkyl or CN) or salt thereof comprising reacting a compound of formula (B)
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- (wherein R1 and R2 are as hereinbefore defined) or a salt thereof with a copper and/or silver compound in the presence of palladium or a compound thereof:
A process for the preparation of a compound of formula (F)
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- (Wherein R2 Represents COOH, COO—C1-6 Alkyl or CN and R3 represents hydrogen, mesylate, triflate, tosylate or carboxy-C1-6-alkyl) or a salt thereof
- comprising reacting a compound of formula (E)
- 19
- (Wherein R2 and R3 are as hereinbefore defined and R4 represents a halogen atom) or a salt thereof
- with azacyclonol.
A compound of formula (E), (G) or (F) or a salt thereof.
A process for the preparation of a compound of formula (H)
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- comprising reacting a compound of formula (D)
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- (wherein R4 is a halogen atom) with azacyclonol.
A pharmaceutical composition comprising a compound of formula (E), (G) or (F) or a salt thereof along with at least one pharmaceutical excipient or carrier.
Dependencies are inferred from the claim text.