Process for the preparation of 4"-amino avermectin compounds

Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives

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C07H 1704, A61K 3170

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053628632

ABSTRACT:
A 4"-oxoavermectin intermediate is reductively aminated using hexa- or heptamethyldisilazane and sodium borohydride to produce a 4"-amino (or methylamino)avermectin. The 4"- aminoavermectin is a useful intermediate in the preparation of N-acyl derivatives. The compounds are useful as agricultural and animal health insecticides and parasiticides.

REFERENCES:
patent: 4427663 (1984-01-01), Mrozik
patent: 4874749 (1989-10-01), Mrozik
patent: 5008191 (1991-04-01), Okazaki et al.
patent: 5212322 (1993-05-01), Okazaki et al.
Pure & Appl. Chem., vol. 62, No. 7, pp. 1231-1240, 1990, by M. H. Fisher.

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