"4""-Keto-and 4""-amino-4""-deoxy avermectin compounds and substituted amino derivatives thereof"
US4427663A · kind A · utility
Assignee
Inventor
Key dates
| Filing date | Mar 16, 1982 |
| Grant date | Jan 24, 1984 |
| Priority date | — |
| Expiry date | Mar 16, 2002 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P33/00
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.