Process for the preparation of azithromycin

Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives

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536 71, 536 72, 514 29, C07H 1708

Patent

active

060137789

ABSTRACT:
The present invention describes a new process for the preparation of azithromycin from a suitable imino ether as precursor, characterised by the fact that the reduction and the reductive methylation of said imino ether are sequentially carried out with a noble metal catalyst and hydrogen in the presence of formaldehyde, or a source thereof, wherein both reactions can be conducted in the same reaction vessel.

REFERENCES:
patent: 4474768 (1984-10-01), Bright
patent: 4517359 (1985-05-01), Kobrehel et al.
patent: 5686587 (1997-11-01), Yang
Paper E/257/87; Erythromycin Series, Part 13, Synthesis and Structure Elucidation of 10-Dihydro-10-deoxy-11-methyl-11-azaerythromycin; Slobodan Djokie, et al.; 1239-1261.
"Erythromycin Series, Part 11, Ring Expansion of Erythromycin A Oxime by the Beckmann Rearrangement"; J. Chem Soc. Perkin Trans. 1 1986; Slobodan Djokie, et al.; 1881-1890.

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