Process for the preparation of 3,4-di-isobutyryloxy-n-...

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260/489.7

B01J 23/44 (2006.01)

Patent

CA 1228367

ABSTRACT OF THE DISCLOSURE A new process is provided herein for the preparation of the therapeutically active compound, 3,4-di-isobutyryloxy-N-methyl- phenethylamine of Formula (I) Image (I) or its pharmaceutically-acceptable acid addition salts. According to the novel process, 3,4-dimethoxy-phenethylamine is first reacted with benzaldehyde and formaldehyde in the presence of hydrogen and a catalyst to give a compound of Formula (II) Image (II) . That compound, of Formula (II), is demethylated and is then reacted with isobutyryl chloride in the presence of a base to give a compound of Formula (IV) Image (IV) , Abstract Continued (Page 2) from which the benzyl protecting group is removed by catalytical hydrogenation, whereby the compound of Formula (I) is obtained. The compound of Formula (I), also known as ibopamine, is a well- known cardiac medicine, which is used especially in heart and kidney insufficiency.

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