| 摘要 |
Novel avermectin and milbemycin compound have the formula …<CHEM>… in which the broken line indicates a single or double bond;… R1 is H, -OH, C1-5 alkanoyloxy, or =O 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, C1-5 alkoxy or C1-5 alkanoyloxy;… R4 is H, OH, or …<CHEM>… and… Y is =O, -NH2, -NOH, =N-NH C6H5, =N-NH-CONH2, =N-NH-CSNH2, =NOR5 where R5 is C1-5 alkyl; or are their trisubstituted silyl protected derivatives. The 13-oxo derivatives are prepared from the corresponding 13-hydroxy compounds by oxidizing the 13-position with a suitable oxidizing agent. They serve as intermediate compounds in the preparation of 13-imino and 13-amino derivatives, which are prepared from them by treatment with a primary amino or with an ammonium compound in the presence of a reducing agent, depending on the 13-substituent desired. The 13-keto, imino and amino compounds have utility as anti-parasitic agents and as highly potent insecticides against agricultural pests, and are made into compositions for those uses. |
