发明名称 |
Fluoxetine process from benzoylacetonitrile |
摘要 |
A synthesis of fluoxetine is disclosed. The process begins with benzoylacetonitrile, which is reduced, optionally in the presence of a chiral ligand, to produce the corresponding aminoalcohol, and the amine is carbamoylated without isolation. The alcohol is deprotonated and reacted with 4-chloro- or 4-fluoro benzotrifluoride or with 4-trifluoromethylphenol to provide a carbamate of fluoxetine. The carbamate is reduced with a hydride or with borane to provide fluoxetine free base. The process may be employed for the synthesis of individual enantiomers of fluoxetine.
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申请公布号 |
US6025517(A) |
申请公布日期 |
2000.02.15 |
申请号 |
US19980128319 |
申请日期 |
1998.08.03 |
申请人 |
SEPRACOR INC. |
发明人 |
HILBORN, JAMES WALLACE;JURGENS, ALEX ROGER |
分类号 |
C07C213/02;C07C213/08;C07C215/32;C07C217/48;C07C269/04;C07C269/06;C07C271/16;(IPC1-7):C07C261/00;C07C213/00 |
主分类号 |
C07C213/02 |
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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