Antiparasitic agents

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C - Chemistry, Metallurgy

07

H

C07H 19/01 (2006.01) A01N 43/90 (2006.01) A01N 55/00 (2006.01) A61K 31/70 (2006.01) C07D 493/22 (2006.01) C07F 7/10 (2006.01) C07H 23/00 (2006.01)

Patent

CA 2130664

Avermectin and milbemycin derivatives such as formula (1) having a double bond at the 3-4 position and a cyano substituent at the 3-position have outstanding anthelmintic properties. They may be prepared by allowing an avermectin or milbemycin derivative having a leaving group at the 5-position, or having double bonds at the 2-3 and 4-5 positions and no substituent at the 5-position to react with an ionic cyanide.

Les dérivés de l'avermectine et de la milbémycine ayant une double liaison en position 3-4 et un substituant cyano en position 3 selon la formule (I) ont des propriétés anthelminthiques exceptionnelles. On peut les préparer en faisant réagir avec un cyanure ionique un dérivé de l'avermectine ou de la milbémycine ayant un groupe se prêtant à une réaction 5 ou ayant une double liaison dans les positions 2-3 et 4-5 et pas de substituant en position 5.

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