초록 ▼

There are disclosed novel avermectin compounds wherein the 4″hydroxy group is oxidized to a keto group or replaced with an amino or substituted amino group. The keto compounds are prepared by oxidation with reagents such as oxalyl chloride in dimethylsulfoxide. The amino compounds are prepared from

There are disclosed novel avermectin compounds wherein the 4″hydroxy group is oxidized to a keto group or replaced with an amino or substituted amino group. The keto compounds are prepared by oxidation with reagents such as oxalyl chloride in dimethylsulfoxide. The amino compounds are prepared from the ketone using a reducing agent and an aminating agent. Substituted amino compounds are prepared from the thus produced unsubstituted amino compounds. The keto compounds and amino compounds have utility as anti-parasitic agents and compositions for that use are also disclosed. The compounds are also highly potent insecticides against agricultural pests. In addition the amino compounds have anti-bacterial activity which is not found in any of the precursors.

대표청구항 ▼

A compound having the formula: [Figure] wherein R1 is 〓O, －NR5R6 or [Figure] wherein R1′is 〓O or －NR5R6: R5 and R6 are independently hydrogen, loweralkyl, loweralkanoyl, substituted benzenesulfonyl wherein the substituent is halogen; or loweralkyl sulfonyl; R2 is hydrogen or hydroxy; R3 is sec-butyl

A compound having the formula: [Figure] wherein R1 is 〓O, －NR5R6 or [Figure] wherein R1′is 〓O or －NR5R6: R5 and R6 are independently hydrogen, loweralkyl, loweralkanoyl, substituted benzenesulfonyl wherein the substituent is halogen; or loweralkyl sulfonyl; R2 is hydrogen or hydroxy; R3 is sec-butyl or iso-propyl; R4 is hydroxy or methoxy; and the broken line indicates a single or a double bond at the 22,23-position provided that R2 can only be hydroxy when the broken line indicates a single bond. A method for the treatment of helminthiasis which comprises administering to an animal infected with helminths an effective amount of a compound of claim 1.