C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 17/08 (2006.01)
Patent
CA 2399634
The invention provides a process for the preparation of 9-deoxo-8a-aza-8a-homoerythromycin A (see formula V) and of its 8a-alkylated derivatives from 9-deoxo-9(Z)--hydroxyiminoerythromycin A via a stereospecific Beckmann rearrangement in a reaction mixture using pyridine as main solvent, resulting in imidate intermediates which are not isolated from said mixture and which are employed directly in a reduction stage using a sufficient amount of borohydride, after extraction of the pyridine with a hydrocarbon which is miscible with the latter and in which said imidates are insoluble. The compound V can be directly N-alkylated at the 8a-position using an aldehyde without being isolated from the reduction mixture.
The invention provides a process for the preparation of 9-deoxo-8a-aza-8a-homoerythromycin A and of its 8a-alkylated derivatives from 9-deoxo-9(Z)- hydroxyiminoerythromycin A via a stereospecific Beckmann rearrangement in a reaction mixture using pyridine as main solvent, resulting in imidate intermediates which are not isolated from said mixture and which are employed directly in a reduction stage using a sufficient amount of borohydride, after extraction of the pyridine with a hydrocarbon which is miscible with the latter and in which said imidates are insoluble. The compound V can be directly N-alkylated at the 8a-position using an aldehyde without being isolated from the reduction mixture.
Leon Patrick
Lhermitte Frederic
Oddon Gilles
Pauze Denis
Merial
Smart & Biggar
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