3633. Eprinomectin
Nomenclature
CAS number: 123997-26-2
(4″R)-4″-(Acetylamino)-4″-deoxyavermectin B1; MK-397; Eprinex (Merck & Co.). Description and references
Mixture of semisynthetic avermectins, q.v.; containing 90% or more of component B1a and 10% or less of component B1b. Prepn: H. H. Mrozik, US 4427663 (1984 to Merck & Co.). Synthesis: R. J. Cvetovich et al., J. Org. Chem. 59, 7704 (1994) and biological activity: T. K. Jones et al., J. Agric. Food Chem. 42, 1786 (1994). Mechanism of action study: J. P. Arena et al., J. Parasitol. 81, 286 (1995).
Properties
Crystalline solid, mp 163.3-165.7°. LD50 orally in mice: 24 mg/kg (Jones).Derivative
Component B1a.Nomenclature
CAS number: 133305-88-1
(4″R)-4″-(Acetylamino)-5-O-demethyl-4″-deoxyavermectin
A1a. C50H75NO14; mol wt 914.13.
C 65.69%, H 8.27%, N 1.53%, O 24.50%.
Derivative
Component B1b.Nomenclature
CAS number: 133305-89-2
(4″R)-4″-(Acetylamino)-5-O-demethyl-25-de(1-methylpropyl)-4″-deoxy-25-(1-methylethyl)avermectin
A1a. C49H73NO14; mol wt 900.10.
C 65.38%, H 8.17%, N 1.56%, O 24.89%.