发明名称 13-ESTER DERIVATIVE OF MILBEMYCINS AND USE THEREOF
摘要 NEW MATERIAL:A 13-ester derivative of a milbemycin shown by formula I (X is H, hydroxyl group or oxo; dotted line is double bond or single bond and is double bond only when X is H; R<1> is 1-8C alkyl, 2-8C alkenyl or alkynyl; R<2> is 1-6C alkyl or 1-4C haloalkyl; R<3> is H or 1-4C alkyl or R<2> and R<3> are bonded to form 2-5C cycloalkylene group; R<4> is H or ester-forming carboxylic acid residue; W is methylene, O or S; n is 0 or 1; A is phenyl or naphthyl). EXAMPLE:13-(2-Methyl-phenylpropionyloxy)milbemycin A<4>. USE:Useful as an acaricide, insecticide and vermicide. Also useful as a drug against parasites infecting human. Capable of being administered orally. PREPARATION:For example, a compound shown by formula II is reacted with a carboxylic acid shown by formula III preferably in the presence of a dehydrating agent to give a compound shown by formula I.
申请公布号 JPH01104078(A) 申请公布日期 1989.04.21
申请号 JP19870068340 申请日期 1987.03.23
申请人 SANKYO CO LTD 发明人 SATO KAZUO;YANAI TOSHIAKI;OTO TAKAO;TANAKA KEIJI;TOYAMA TOSHIMITSU
分类号 A01N43/90;A01N47/06;A61K31/365;A61K31/38;A61K31/415;A61K31/42;A61K31/44;A61K31/445;A61K31/495;A61P33/00;A61P33/10;C07D493/22 主分类号 A01N43/90
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