Process for the preparation of (8s)-8- fluoroerythromycins

Details Process for the preparation of (8s)-8- fluoroerythromycins Process for the preparation of (8s)-8- fluoroerythromycins

C - Chemistry, Metallurgy

07

H

260/230.3

C07H 17/08 (2006.01)

Patent

CA 1223253

ABSTRACT OF THE DISCLOSURE For the synthesis of (8S)-8-fluoroerythromycins the corresponding 8,9-anhydroerythromycins 6,9-hemiketal are directly fluorinated with perchloryl fluoride. The process of the present invention permits erythromycin (or the deri- vative thereof 8,9-anhydroerythromycin 6,9-hemiketal) to be directly converted into (8S)-8-fluoroerythromycin without it being necessary to protect the N-dimethyl group of the desosamine during the fluorination and without the necessity of carrying out a subsequent step of methylating hydrogena- tion.

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