Process for the glycosylation of avermectin compounds

Details Process for the glycosylation of avermectin compounds Process for the glycosylation of avermectin compounds

C - Chemistry, Metallurgy

12

P

C12P 19/62 (2006.01) A01N 43/90 (2006.01) A01N 63/02 (2006.01) C07H 17/08 (2006.01) C07H 19/01 (2006.01) C12P 19/60 (2006.01) A61K 31/71 (1990.01)

Patent

CA 2071574

102/DLR52 18437 TITLE OF THE INVENTION A PROCESS FOR THE GLYCOSYLATION OF AVERMECTIN COMPOUNDS ABSTRACT OF THE DISCLOSURE Avermectin compounds are glycosylated the 4' and 4"-positions by adding the avermectin compounds to the fermentation medium of Saccharapolyspora erythera. The outer oleandrose sugar group of the avermectin compound is glycosylated with a glycosyl moiety, specifically a glucose group. In addition, other changes are effected in the avermectin moiety such as selective hydroxylation, epimerization at the 2-carbon and migration of the .DELTA. 3-double bond to a .DELTA. 2-position.

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