Process for the manufacture of 3-amino-5- methylisoxazole

C - Chemistry – Metallurgy – 07 – D

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260/311.9

C07D 261/14 (2006.01)

Patent

CA 1301766

ABSTRACT OF THE DISCLOSURE An improved process for the manufacture of 3-amino-5- methylisoxazole is described. According to the process a nitrile compound selected from the group consisting of 2,3-dibromo- butyronitrile, 2-bromo-3-methoxybutyronitrile, 2-bromocrotono- nitrile and tetrolonitrile or mixtures thereof is reacted with hydroxyurea in the medium of an alkali metal hydroxide, wherein the pH during the reaction is maintained in the range of between 10.1 to 13 and preferably between 10.5 to 12.5. Optionally, an inert organic solvent is also present in the reaction system. The hydroxyurea may be also prepared in-situ from alkyl carbamate and hydroxyamine in an aqueous alkali medium. The 3-amino-5- methylisoxazole derivatives are useful intermediates for the synthesis of sulfa drugs.

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