发明名称 |
PRODUCTION OF AVERMECTIN COMPOUNDS |
摘要 |
<p>This invention provides a process for preparing a compound of formula (I): wherein R<1> is H or a hydroxyimino-protecting group; R<2> is H, C1-4 alkyl or C1-4 alkoxy; R<3> is C1-8 alkyl, C2-8 alkenyl or C3-8 cycloalkyl; and R<4> is H, halo, C1-4 alkyl or C1-4 alkoxy, which process comprises the steps of: (a) reacting an avermectin B2 derivative with an oxidizing agent to form a 5-oxo compound; (b) allowing the 5-oxo compound to react with a compound of formula R<1>-O-NH2 wherein R<1> is H or a hydroxyimino-protecting group, to form a 5-imino compound; (c) reacting the 5-imino compound with a thionocarbonizing agent to form a 4'', 23-bisthionocarbonyl ester; (d) reacting the 4'', 23-bisthionocarbonyl ester with a deoxygenation agent to form a 4'', 23-dideoxy compound; and (e) reacting the 4'', 23-dideoxy compound with an acid to form a compound of formula (I).</p> |
申请公布号 |
WO9905156(A1) |
申请公布日期 |
1999.02.04 |
申请号 |
WO1998IB00988 |
申请日期 |
1998.06.25 |
申请人 |
PFIZER PHARMACEUTICALS INC.;PFIZER INC.;HONDA, MASANORI;KADOI, HIROSHI;MORITA, HIROMASA;NAGAKURA, ISAO |
发明人 |
HONDA, MASANORI;KADOI, HIROSHI;MORITA, HIROMASA;NAGAKURA, ISAO |
分类号 |
A61K31/7048;A61P33/10;C07H17/08;C07H19/01;(IPC1-7):C07H19/01;A61K31/70 |
主分类号 |
A61K31/7048 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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