Method for producing 3-substituted...

C - Chemistry – Metallurgy – 07 – D

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C07D 213/803 (2006.01) C07D 213/85 (2006.01)

Patent

CA 2521695

A method for producing a 3-substituted 2-chloro-5-fluoro-pyridine or its salt in high yield from a readily available material through a short process under mild reaction conditions using a reagent which is easy for handling and simple in the reaction operation. The method comprising selectively reducing a chlorine atom at the 6-position of the following compound (1) or its salt, to obtain the following compound of formula (2) or its salt. The compound of formula (2) or its salt may be further substituted to obtain the following compound (4) or its salt. Here, Z1 is -CO2R1, etc., Z2 is a group different from Z1 and is -CO2R5, etc. R1 and R5 are independently an alkyl group, an alkenyl group, an aryl group, an aralkyl group or cycloalkyl group, or R1 is hydrogen. (see formula 1) (see formula 2) (see formula 4)

L'invention concerne des méthodes de production en grande quantité de 2-chloro-5-fluoropyridine 3-substitué ou de son sel à partir d'un matériau facile à obtenir, par une étape courte, dans des conditions de réaction douces, au moyen d'un réactif simple à mettre en réaction et facile à gérer. Une des méthodes est un procédé de production du composé (2) ou de son sel, qui consiste à réduire le composé (1) ou son sel sélectivement au niveau de l'atome de chlore en position 6. L'autre méthode est un procédé de production du composé (4) ou de son sel, qui consiste à remplacer le groupe Z?1¿ du composé (2) ou son sel obtenu par la réaction de réduction par le groupe Z?2¿. Dans les formules suivantes, Z?1¿ représente CO¿2?R?1¿, etc. (R?1¿ étant hydrogène, alkyle, alcényle, aryle, aralkyle ou cycloalkyle); et Z?2¿ est un groupe différent de Z?1¿ et CO¿2?R?5¿, etc (R?5¿ étant alkyle, alcényle, aryle, aralkyle ou cycloalkyle).

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