394222-36-7

Upstream product

• 129488-73-9 methyl 4-(1-cyano-1-methylethyl)-benzoate 
• 394222-38-9 2-(4-(4-bromobutanoyl)phenyl)-2-methylpropanenitrile 
• 115-46-8 C₁₈H₂₁NO 
• 1252902-28-5 4-(4-(2-cyanopropan-2-yl)phenyl)-4-oxobutyl 4-methylbenzenesulfonate 
• 1308679-43-7 C₁₅H₁₄NO₃^(1-)*Na⁽¹⁺⁾ 
• 394222-37-8 2-(4-(4-hydroxybutanoyl)phenyl)-2-methylpropanenitrile 
• 169032-17-1 2-[4-(4-chloro-butyryl)-phenyl]-2-methyl-propionitrile 
• 76469-88-0 methyl 4-(cyanomethyl)benzoate 
• 169280-06-2 2-(4-cyclopropanecarbonyl-phenyl)-2-methyl-propionitrile 
• 252022-33-6 2-[4-(4-Hydroxy-1-butynyl)phenyl]isobutyronitrile 
• 101184-73-0 2-(4-bromophenyl)-2-methylpropanenitrile 
• 252022-35-8 2-[4-(4-(4-Hydroxydiphenylmethyl-1-piperidyl)-1-butynyl)phenyl]isobutyronitrile 

Downstream Products

• 83799-24-0 fexofenadine 
• 1319714-86-7 fexofenadine sodium salt 
• 138452-21-8 fexofenadine hydrochloride 
• 169032-19-3 2-(4-{1-hydroxy-4-[4-(hydroxydiphenylmethyl)piperidin-1-yl]butyl}phenyl)-2-methylpropionitrile 

Relevant academic research and scientific papers

PROCESS FOR THE PREPARATION OF FEXOFENADINE AND OF INTERMEDIATES USED THEREIN

A new process for the preparation of fexofenadine and of related intermediates, which can be used in the preparation of fexofenadine, is provided.

Processes for the production of fexofenadine

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.

A new synthesis of carboxyterfenadine (fexofenadine) and its bioisosteric tetrazole analogs

A new synthesis of carboxyterfenadine (4), based on the conversion of a α-halo-alkylarylketone into the corresponding substituted 2-arylalkanoic ester, is described. The enantioselective synthesis of its two bioisosteric tetrazole analogs together with preliminary biological results are reported. Copyright (C) 1999 Elsevier Science S.A.