Avermectin and milbemycin 13-keto, 13-imino and 13-amino derivat

Details Avermectin and milbemycin 13-keto, 13-imino and 13-amino derivat Avermectin and milbemycin 13-keto, 13-imino and 13-amino derivat

1984-06-11

1986-04-01

Fan, Jane T.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514409, 548525, 549264, A61K 31365, C07D49320

Patent

active

045798648

ABSTRACT:
There are disclosed novel avermectin and milbemycin compounds wherein the 13-position is oxidized to a keto function. The 13-keto derivatives are prepared from the 13-hydroxy compounds by oxidizing the 13-position with a suitable oxidizing agent. The avermectin and milbemycin 13-keto derivatives are active in their own right and also serve as intermediates in the preparation of 13-imino and 13-amino derivatives. The 13-keto, imino 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.

REFERENCES:
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patent: 4310519 (1982-01-01), Albers-Schonberg et al.
Tetrahedron Letters 24 5333-5336, (1983).

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