Synthesis of terfenadine and derivatives

Details Synthesis of terfenadine and derivatives Synthesis of terfenadine and derivatives

C - Chemistry, Metallurgy

07

D

C07D 317/30 (2006.01) C07C 69/612 (2006.01) C07C 69/738 (2006.01) C07C 69/76 (2006.01) C07D 211/22 (2006.01) C07D 211/34 (2006.01) C07D 307/20 (2006.01) C07D 317/20 (2006.01) C07D 317/22 (2006.01)

Patent

CA 2279960

Processes for preparing compounds having general formula (1), wherein R1a is protected carboxy, carboxy, hydroxymethyl, protected hydroxymethyl, or methyl are disclosed. Processes of the invention begin with a starting material of general formula (II), and elaborate the product by reductive amination of an aldehyde of formula (IVa) with .alpha.,.alpha.-diphenyl-4-piperidinemethanol.

L'invention concerne des procédés pour préparer des composés de formule générale (1), dans laquelle R<1a> représente carboxy protégé, carboxy, hydroxyméthyle, hydroxyméthyle protégé, ou méthyle. Selon les procédés de l'invention, le matériau de départ correspond à la formule générale (II), le produit étant élaboré par amination réductrice d'un aldéhyde de formule IVa, avec un alpha , alpha -diphényl-4-pipéridineméthanol.

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