发明授权
US08637667B2 Method for preparing (S)-5-chloro-N-((3-(4-(5,6-dihydro-4H-1,2,4-oxadiazin-3-yl)phenyl)-2-oxooxazolidin-5-yl)methyl)thiophene-2-carboxamide derivatives
有权
制备（S）-5-氯-N - （（3-（4-（5,6-二氢-4H-1,2,4-恶二嗪-3-基）苯基）-2-氧代恶唑烷-5-基） 噻唑-2-基）甲基）噻吩-2-甲酰胺衍生物
- 专利标题： Method for preparing (S)-5-chloro-N-((3-(4-(5,6-dihydro-4H-1,2,4-oxadiazin-3-yl)phenyl)-2-oxooxazolidin-5-yl)methyl)thiophene-2-carboxamide derivatives
- 专利标题（中）： 制备（S）-5-氯-N - （（3-（4-（5,6-二氢-4H-1,2,4-恶二嗪-3-基）苯基）-2-氧代恶唑烷-5-基） 噻唑-2-基）甲基）噻吩-2-甲酰胺衍生物
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申请号： US13382265申请日： 2010-07-07
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公开(公告)号： US08637667B2公开(公告)日： 2014-01-28
- 发明人: Young Lag Cho , Jong Un Cho , Sung Yoon Baek , Ho Young Song , Tae Kyo Park , Sung Ho Woo , Yong Zu Kim
- 申请人： Young Lag Cho , Jong Un Cho , Sung Yoon Baek , Ho Young Song , Tae Kyo Park , Sung Ho Woo , Yong Zu Kim
- 申请人地址： KR Daejeon
- 专利权人： Legochem Bioscience Ltd.
- 当前专利权人： Legochem Bioscience Ltd.
- 当前专利权人地址： KR Daejeon
- 代理机构： Sughrue Mion, PLLC
- 优先权： KR10-2009-0062122 20090708
- 国际申请： PCT/KR2010/004420 WO 20100707
- 国际公布： WO2011/005028 WO 20110113
- 主分类号： C07D413/02
- IPC分类号： C07D413/02 ; C07D413/04 ; C07D273/04
摘要：
Provided is a method for preparing (S)-5-chloro-N-((3-(4-(5,6-dihydro-4H-1,2,4-oxadiazin-3-yl)phenyl)-2-oxooxazolidin-5-yl)methyl)thiophene-2-carboxamide derivatives of Formula (I) which are useful as blood coagulation factor Xa inhibitors, and said method using 1-fluoro-4-nitrobenzen as a starting material. According to the method of the present invention, (S)-5-chloro-N-((3-(4-(5,6-dihydro-4H-1,2,4-oxadiazin-3-yl)phenyl)-2-oxooxazolidin-5-yl)methyl)thiophene-2-carboxamide derivatives of Formula (I) which are useful as blood coagulation factor Xa inhibitors can be prepared in a high purity and a high yield.