C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 277/56 (2006.01) C07K 5/065 (2006.01)
Patent
CA 2380084
The present invention relates to a process for preparing 2-aminomethyl-4-cyano-thiazole and salts thereof of general formulae (Ia) and (Ib) where n is 1 or 2; when n is 1, then X is chloride, bromide, triflate and hydrogen sulphate; and when n is 2, then X is sulphate. The method involves stirring thioamide of formula (IV) with a bromopyruvic acid ester of formula (V), in which R1 is a linear or branched C1-4, in a R2OH alcohol, wherein R2 is a linear or branched C1-8 alkyl, HO-CH2-CH2-, HO-CH2-CH2-CH2- or C1-4 alkyl-O-CH2-CH2-. Said stirring process is carried out at a temperature of -5°C to 40°C until the reaction of the thioamide of formula (IV) is practically complete. This invention also relates to the compounds of formulae (Ia) and (Ib).
L'invention concerne un procédé de production de 2-aminométhyl-4-cyano-thiazol et de ses sels de formules (Ia) et (Ib), dans laquelle n vaut 1 ou 2 ; lorsque n vaut 1, X représente chlorure, bromure, triflate et sulfate d'hydrogène ; lorsque n vaut 2, X représente sulfate. Ce procédé consiste à agiter le thioamide de formule (IV) avec un ester d'acide bromopyruvique de formule (V), dans laquelle R<1> représente alkyle C1-4 linéaire ou ramifié, dans un alcool R<2>OH, dans lequel R<2> représente alkyle C1-8 linéaire ou ramifié, HO-CH2-CH2-, HO-CH2-CH2-CH2- ou alkyle CH1-4-O-CH2-CH2-, à une température comprise 5 DEG C et 40 DEG C, jusqu'à réaction pratiquement complète du thioamide de formule (IV). L'invention concerne également les composés de formules (Ia) et (Ib).
Abbott Gmbh & Co. Kg
Basf Aktiengesellschaft
Robic
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