发明名称 |
PROCESS FOR PREPARING PYRAZOLE FUNCTIONALIZED BENZODIAZEPINONES |
摘要 |
The present invention provides innovative strategies for synthesizing pyrazole ring- functionalized benzodiazepinones. Alternative intermediates and high conversion strategies for forming alpha-aminobenzophenone intermediates involve a combination of aromatic acylation, displacement of electronegative leaving groups with amine, and then N-displacement strategies to produce the desired alpha-aminobenzophenone with primary amine functionality. Reaction strategies are then provided for converting alpha-aminobenzophenones to alpha- amino amidobenzophenone intermediates with high yield and convenient reaction strategies. These alpha-aminoamidobenzophenone intermediates are then converted into benzodiazepinones. These benzodiazepinones are then converted to pyrazole ring functionalized benzodiazepinones through a series of innovative intermediates and/or reaction strategies. |
申请公布号 |
WO2009100996(A2) |
申请公布日期 |
2009.08.20 |
申请号 |
WO2009EP51138 |
申请日期 |
2009.02.02 |
申请人 |
F. HOFFMANN-LA ROCHE AG;HARRINGTON, PETER JOHN;PAULSEN, VALERIE GRACE;TUCKER, CHARLES E. |
发明人 |
HARRINGTON, PETER JOHN;PAULSEN, VALERIE GRACE;TUCKER, CHARLES E. |
分类号 |
C07D243/24;C07C221/00;C07C225/22;C07C237/04;C07D243/28;C07D487/04 |
主分类号 |
C07D243/24 |
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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