发明名称 |
Procedure for the inversion of the stereochemistry at C13 of avermectin aglycone compounds. |
摘要 |
<p>The natural stereochemistry at the 13-position of avermectin aglycones, normally alpha -oriented or below the plane of the molecule, is inverted or epimerized into the beta -position. The procedure starts with the avermectin aglycone compounds where the 13 alpha -hydroxy group is substituted with a leaving group. Treatment of the substituted compound with tetra alkyl ammonium nitrate displaces the leaving group, substitutes a nitrate ester or a nitrooxy group, for the hydroxy and inverts the 13-stereochemistry to beta . Reduction of the nitrooxy group returns the 13-hydroxy group and retains the 13- beta configuration. The intermediate 13-nitrooxy compounds are themselves potent anti-parasitic agents.</p> |
申请公布号 |
EP0514090(A1) |
申请公布日期 |
1992.11.19 |
申请号 |
EP19920304151 |
申请日期 |
1992.05.08 |
申请人 |
MERCK & CO. INC. |
发明人 |
JONES, TODD K.;MROZIK, HELMUT |
分类号 |
C07D493/22;A01N43/90;A61K31/365;A61P33/00;A61P33/10;C07H19/01 |
主分类号 |
C07D493/22 |
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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