发明公开
- 专利标题： Synthesis of benzoquinolinones
- 专利标题（中）： 苯并喹啉酮的合成
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申请号： EP95303422.0申请日： 1995-05-23
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公开(公告)号： EP0684234A1公开(公告)日： 1995-11-29
- 发明人: Audia, James Edmund , Droste, James Joseph , Heath, Perry Clark , Weigel, Leland Otto
- 申请人： ELI LILLY AND COMPANY
- 申请人地址： Lilly Corporate Center Indianapolis, Indiana 46285 US
- 专利权人： ELI LILLY AND COMPANY
- 当前专利权人： ELI LILLY AND COMPANY
- 当前专利权人地址： Lilly Corporate Center Indianapolis, Indiana 46285 US
- 代理机构： Hudson, Christopher Mark
- 优先权： US249582 19940526
- 主分类号： C07D221/10
- IPC分类号： C07D221/10 ; C07C211/42
摘要：
A process for preparing 10b-methyl-3-oxo-benzo[f] quinolines of the formula
wherein R is hydrogen, methylthio, chloro, bromo or fluoro, and is located at the 7-, 8- or 9-position; comprising reacting a compound of the formula
with methyl iodide in an ether solvent to prepare a compound of the formula
combining acrylic anhydride or acryloyl chloride with the reaction mixture comprising the compound of formula III to prepare a compound of the formula
quenching the reaction with sodium bicarbonate, evaporating the organic solution comprising the compound of formula IV;
and combining the residue comprising the compound of formula IV with a trialkylsilane and trifluoroacetic acid in the absence of a solvent to prepare the compound of formula I.
wherein R is hydrogen, methylthio, chloro, bromo or fluoro, and is located at the 7-, 8- or 9-position; comprising reacting a compound of the formula
with methyl iodide in an ether solvent to prepare a compound of the formula
combining acrylic anhydride or acryloyl chloride with the reaction mixture comprising the compound of formula III to prepare a compound of the formula
quenching the reaction with sodium bicarbonate, evaporating the organic solution comprising the compound of formula IV;
and combining the residue comprising the compound of formula IV with a trialkylsilane and trifluoroacetic acid in the absence of a solvent to prepare the compound of formula I.
公开/授权文献
- EP0684234B1 Synthesis of benzoquinolinones 公开/授权日：2000-07-26
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