4"-Keto-and 4"-amino-4"-deoxy avermectin compounds and substitut

Details 4"-Keto-and 4"-amino-4"-deoxy avermectin compounds and substitut 4"-Keto-and 4"-amino-4"-deoxy avermectin compounds and substitut

1982-03-16

1984-01-24

Brown, Johnnie R.

Drug, bio-affecting and body treating compositions

Conjugate or complex of monoclonal or polyclonal antibody,...

Conjugated via claimed linking group, bond, chelating agent,...

536 71, 424181, A61K 3171, C07H 1522

Patent

active

044276630

ABSTRACT:
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.

REFERENCES:
patent: 4044123 (1977-08-01), Daniels et al.
patent: 4085119 (1978-04-01), Myers
patent: 4090017 (1978-05-01), Sciavolino
patent: 4098993 (1978-07-01), Bright
patent: 4107435 (1978-08-01), Ross
patent: 4133950 (1979-01-01), Myers
patent: 4199569 (1980-04-01), Chabala et al.
patent: 4206205 (1980-06-01), Mrozik et al.
patent: 4310519 (1982-01-01), Albers-Schonberg et al.
Chemical Abstracts 91: 175223f to Bright (II).
Chemical Abstracts 90: 23614a to Sciavolino (II).
Chemical Abstracts 90: 23615b to Sciavolino (III).

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