| 摘要 |
<p>Novel avermectin and milbemycin phosphate esters have the formula:
<CHEM>
where the broken line indicates a single or a double bond;
R1 is H, loweralkanoyloxy, OH = O or OR provided that R1 is present only when the broken line indicates a single bond;
R2 is methyl, ethyl, iso-propyl or sec-butyl;
R3 is OH, OCH3, loweralkanoyloxy, or OR;
R4 is H, OH, OR, loweralkanoyloxy, alpha -L-oleandrosyl-oxy, 4 min -( alpha -L-oleandrosyl)- alpha -L-oleandrosyloxy,
4 min -loweralkanoyl- alpha -L-oleandrosyloxy, 4 sec -loweralkanoyl-4 min -( alpha -L-oleandrosyl)- alpha -L-oleandrosyloxy,
<CHEM>
R5 is H, or OR; and
H is P(O) (OH) (OMe), P(O) (OMe)2, P(O) (OCH2CCl3)2, P(O) (OH)2, P(O) (OH) (OM), P(O) (OM)2, P(O) (OH)-O (N3N<+>-alk), P(O) (O )2 (H3N<+>alk)2,
where M is an alkali metal, Me is methyl and alk is C1-5 alkyl; and physiologically acceptable salts thereof; and <<lower alkanoyloxy>> means <<C1-5 alkanoyloxy>>, either straight or branched chain; and with the proviso that at least one or R1, R3, R4 and R5 is an OR residue. These phosphate esters are prepared by reacting an avermectin or milbemycin compound with one or more unprotected hydroxy groups with a disubstituted halo phosphate. They have increased water-solubility when compared with the parent compounds. They have utility as anti-parasitic agents and may be made into compositions for that use. They are also highly potent insecticides against certain agricultural pests. </p> |
