发明公开
EP1057810A1 Method for producing n-protected-azetidine-2-carboxylic acids
审中-公开
Verfahren zur Herstellung von N-geschütztenAzetidin-2-Carbonsaüren
- 专利标题： Method for producing n-protected-azetidine-2-carboxylic acids
- 专利标题（中）： Verfahren zur Herstellung von N-geschütztenAzetidin-2-Carbonsaüren
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申请号： EP00111694.6申请日： 2000-05-31
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公开(公告)号： EP1057810A1公开(公告)日： 2000-12-06
- 发明人: Yamauchi, Kazuhiro , Ushio, Hideki , Kurimoto, Isao
- 申请人： Sumitomo Chemical Company, Limited
- 申请人地址： 5-33, Kitahama 4-chome Chuo-ku Osaka 541-8550 JP
- 专利权人： Sumitomo Chemical Company, Limited
- 当前专利权人： Sumitomo Chemical Company, Limited
- 当前专利权人地址： 5-33, Kitahama 4-chome Chuo-ku Osaka 541-8550 JP
- 代理机构： Henkel, Feiler, Hänzel
- 优先权： JP15375299 19990601
- 主分类号： C07D205/04
- IPC分类号： C07D205/04
摘要：
There is disclosed a method for producing an essentially enantiomerically pure N-protected-azetidine-2-carboxylic acid of formula (I):
which method is characterized by:
subjecting a crude enantiomerically excess N-protected-azetidine-2-carboxylic acid comprising said enantiomer represented by formula (1) in excess to the other enantiomer thereof to crystallization in an organic solvent selected from aromatic hydrocarbon, aliphatic ether, aliphatic alcohol, aliphatic ketone, aliphatic nitrile, aliphatic amide, aliphatic sulfoxide, aliphatic ester and a mixed solvent thereof,
wherein R is:
an optionally substituted alkyl, alicyclic or alicyclicalkyl group,
an optionally substituted alkenyl group,
an optionally substituted aryl group,
an optionally substituted heteroaryl group, or
a dialkylamino group and
absolute configuration of the asterisked asymmetric carbon atom is S or R .
which method is characterized by:
subjecting a crude enantiomerically excess N-protected-azetidine-2-carboxylic acid comprising said enantiomer represented by formula (1) in excess to the other enantiomer thereof to crystallization in an organic solvent selected from aromatic hydrocarbon, aliphatic ether, aliphatic alcohol, aliphatic ketone, aliphatic nitrile, aliphatic amide, aliphatic sulfoxide, aliphatic ester and a mixed solvent thereof,
wherein R is:
an optionally substituted alkyl, alicyclic or alicyclicalkyl group,
an optionally substituted alkenyl group,
an optionally substituted aryl group,
an optionally substituted heteroaryl group, or
a dialkylamino group and
absolute configuration of the asterisked asymmetric carbon atom is S or R .
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