Process for producing erythromycin derivative

Details Process for producing erythromycin derivative Process for producing erythromycin derivative

C - Chemistry, Metallurgy

07

H

C07H 17/08 (2006.01) C07H 1/00 (2006.01)

Patent

CA 2417319

A method of introducing a 6-position substituent into a 6,9-cyclic acetal of a 5-O-desosaminylerythronolide derivative, characterized by cleaving the cyclic acetal selectively at the 9-position C-O bond; and a process for efficiently synthesizing a 6-O-substituted ketolide derivative which comprises a combination of conversion of each of the 9- and 3-position substituents into a carbonyl group and formation of a 11,12-cyclic carbamate.

Procédé servant à introduire un substituant de position 6 dans un acétal 6,9-cyclique d'un dérivé de 5-O-desosaminylérythronolide, ce qui consiste à cliver l'acétal cyclique de façon sélective au niveau de la liaison C-O en position 9. Procédé de synthèse d'un dérivé de cétolide 6-O-substitué, ce qui consiste à combiner la conversion de chacun des substituants de position 9 et 3 dans un groupe carbonyle et la formation d'un carbamate 11,12-cyclique.

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