Synthesis of pharmaceutically useful pyridine derivatives

Details Synthesis of pharmaceutically useful pyridine derivatives Synthesis of pharmaceutically useful pyridine derivatives

C - Chemistry, Metallurgy

07

D

C07D 401/12 (2006.01) C07D 213/61 (2006.01) C07D 213/68 (2006.01) C07D 213/78 (2006.01) C07D 213/803 (2006.01) C07D 213/81 (2006.01)

Patent

CA 2204580

A process is provided for the preparation of compounds of formula I, (see fig. I) useful in the preparation of compounds such as Omeprazole, Lansoprazole and Pantoprazole, wherein R1=H or CH3, R2=H or CH3, R3=Alkoxy (1-4C), OCH2CF3, Cyano, Hydrogen, Halogen, Acetoxy or Aryloxy, any electron withdrawing group or salts (organic or inorganic) of electron donating groups, R=Alkoxy, Hydroxy, Halogen, Activated ester, Tosylate, Mesylate, Thiol or Xanthyl, wherein the process for the preparation of compound of formula I employs a free radical reaction to functionalize the 2-position.

Divulgation d'un procédé de préparation de composés de formule I, (voir fig. I), utiles pour la préparation de composés comme l'Oméprazole, le Lansoprazole et le Pantoprazole, dans laquelle R1 est un H ou un CH3, R2 est un H ou un CH3, R3 est un alcoxy en C1-4, OCH2CF3, un groupement cyano, un hydrogène, un halogène, un acétoxy ou un aryloxy, tout groupe arrachant des électrons ou un sel (organique ou inorganique) de groupes donneurs d'électrons, R est un alcoxy, un hydroxy, un halogène, un ester activé, un tosylate, un mésylate, un thiol ou un xanthyle. Le procédé de préparation du composé de formule I fait intervenir une réaction avec un radical libre pour placer un groupement fonctionnel en position 2.

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