New process for the preparation of...

C - Chemistry – Metallurgy – 07 – C

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C07C 213/02 (2006.01) C07C 217/84 (2006.01)

Patent

CA 2649615

A process for the preparation of 4-hydroxyalkylamino-2-nitro-anisoles of the general formula (I) wherein m is 2 or 3; by reaction of a 4-halogeno-3-nitro-aniline of formula (II) with a chloroalkyl-chloroformate of formula (III), alkaline ring closure of the resulting carbamate and nucleophilic replacement of the halogeno atom by a methoxy group to form a derivative of formula (IV), and finally ring opening of the resulting cyclic carbamate by treatment with methanolic alkali metal hydroxide, followed by neutralization with inorganic or organic acids, wherein the complete reaction is executed in a non-aqueous medium; as well as process for the preparation of 2-amino-4- hydroxyalkylamino-anisoles of formula (V).

L'invention concerne un procédé pour préparer des 4-hydroxyalkylamino-2-nitro-anisoles de formule générale (I) dans laquelle m représente 2 ou 3, par : réaction d'une 4-halogéno-3-nitro-aniline de formule (II) avec un chloroalkyl-chloroformiate de formule (III); fermeture du cycle alcalin du carbamate obtenu, et substitution nucléophile de l'atome halogéno par un groupe méthoxy pour former un dérivé de formule (IV), et; ouverture du cycle du carbamate cyclique obtenu, par traitement au moyen d'un hydroxyde de métal alcalin méthanolique, puis neutralisation à l'aide d'acides inorganiques ou organiques, la réaction complète étant réalisée en milieu non aqueux. La présente invention concerne en outre un procédé pour préparer des 2-amino-4- hydroxyalkylamino-anisoles de formule (V).

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