C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 213/85 (2006.01) A61K 31/44 (2006.01) C07B 39/00 (2006.01)
Patent
CA 2285365
The invention relates to 2,6-dichloro-5-fluoronicotinitrile which can be advantageously obtained by reacting 3-cyano-2-hydroxy-5-fluoropyride-6-one and/or its tautomers and/or its salts and/or their tautomers with phosphorus trichloride and chloric gas in a solvent with addition of a basic catalyst at temperatures between 30 and 300 ~C, and then by hydrolysis. The 3-cyano-2- hydroxy-5-fluoropyride-6-one-monosodium salt which can be used is a new chemical compound that is easy to obtain from 3-cyano-2-hydroxy-5-fluoropyride- 6-one and/or its tautomers by reaction with alcoholate and precipitation with a moderately weak acid.
L'invention concerne du 2,6-dichloro-5-fluoroniconitrile pouvant être avantageusement obtenu par réaction de 3-cyano-2-hydroxy-5-fluoropyride-6-one et/ou ses tautomères et/ou ses sels et/ou leurs tautomères avec du trichlorure de phosphore et du chlore gazeux dans un solvant, sous adjonction d'un catalyseur basique à des températures comprises entre 30 et 300 ·C, puis par hydrolyse. Le 3-cyano-2-hydroxy-5-fluoropyride-6-one-sel monosodique à utiliser est un nouveau composé chimique facile à obtenir à partir de 3-cyano-2-hydroxy-5-fluoropyride-6-one et/ou ses tautomères, par réaction avec de l'alcoolat et par précipitation avec de l'acide modérément faible.
Griehsel Bernd
Sattler Andreas
Steffan Guido
Aktiengesellschaft Bayer
Fetherstonhaugh & Co.
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