Title:
13BETA-O-METHOXYMETHYL-22,23-DIHYDROAVERMECTIN B1A/B1B AGLYCONE AS SUPERIOR ANTIPARASITIC AGENT
Document Type and Number:
Japanese Patent JPH05213958
Kind Code:
A
Abstract:
PURPOSE: To provide a new compd. having excellent long-term duration and useful as an antiparasitic agent and anthelmintic.
CONSTITUTION: This compd. is expressed by formula I, wherein R is sec-butyl or isopropyl, and the compd. is, for example, 13β-O-methoxymethyl-22,23- dihydroavermectin BIa/BIb aglycone. The compd. of formula I is obtd. by allowing an avermectin aglycone expressed by formula II to react with a halomethyl ether expressed by CH3OCH2Cl, especially chloromethyl methyl ether in the presence of a base (e.g. triethylamine) in an anhydrous aprotic solvent (e.g. methylene chloride) at 10 to 120°C for 12 to 24 hours. The avermectin is obtd. by isolating from a fermentation soln. of Streptomyces avermitilis or its deriv.
Inventors:
BURUUSU OO RIN
HERUMUUTO MUROTSUIKU
HERUMUUTO MUROTSUIKU
Application Number:
JP22998892A
Publication Date:
August 24, 1993
Filing Date:
August 28, 1992
Export Citation:
Assignee:
MERCK & CO INC
International Classes:
A61K31/35; A01N43/90; A61P33/00; A61P33/10; C07D493/22; C07H19/01; (IPC1-7): A61K31/35; C07D493/22
Domestic Patent References:
JPS61200993A | 1986-09-05 |
Attorney, Agent or Firm:
Yoshio Kawaguchi (2 outside)
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