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公开(公告)号：US10364219B2
公开(公告)日：2019-07-30
申请号：US15835649
申请日：2017-12-08
发明人： Hua Bai , Xuyang Zhao , Yuncai Zhang , Xufei Li , Yong Zhang , Dezhou Xu , Li Zhang , Xiaojie Xu , Qifeng Zhu , Xiaoming Wang , Zhiqing Yang , Zehua Zhong , Jian Zhang
IPC分类号： C07D205/08 , C07C67/30 , C07C67/343 , C07C69/65 , C07C69/732 , C07C51/367 , C07C59/56 , C07C67/327
摘要： Disclosed is a new method for preparing an azetidinone compound represented by formula (I). The carboxylic ketoester represented by formula (II) serves as the raw material and is subjected to Grignard addition, stereoselective dehydration, ester group reduction, hydroxyl group protection, addition with imine after condensation with a chiral auxiliary, cyclization and deprotection to obtain the compound represented by formula (I). The present invention has advantages of easily available raw material, a few synthetic steps, simple operation, high yield, good stereoselectivity and low cost, and can be used for industrial production.
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公开(公告)号：US20180099930A1
公开(公告)日：2018-04-12
申请号：US15835649
申请日：2017-12-08
发明人： Hua Bai , Xuyang Zhao , Yuncai Zhang , Xufei Li , Yong Zhang , Dezhou Xu , Li Zhang , Xiaojie Xu , Qifeng Zhu , Xiaoming Wang , Zhiqing Yang , Zehua Zhong , Jian Zhang
IPC分类号： C07D205/08 , C07C59/56 , C07C51/367 , C07C67/327 , C07C69/65 , C07C67/343 , C07C67/30 , C07C69/732
CPC分类号： C07D205/08 , C07C51/367 , C07C59/56 , C07C67/30 , C07C67/327 , C07C67/343 , C07C69/65 , C07C69/732
摘要： Disclosed is a new method for preparing an azetidinone compound represented by formula (I). The carboxylic ketoester represented by formula (II) serves as the raw material and is subjected to Grignard addition, stereoselective dehydration, ester group reduction, hydroxyl group protection, addition with imine after condensation with a chiral auxiliary, cyclization and deprotection to obtain the compound represented by formula (I). The present invention has advantages of easily available raw material, a few synthetic steps, simple operation, high yield, good stereoselectivity and low cost, and can be used for industrial production.
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公开(公告)号：US09926268B2
公开(公告)日：2018-03-27
申请号：US15317297
申请日：2015-06-05
发明人： Hua Bai , Xuyang Zhao , Yuncai Zhang , Xufei Li , Yong Zhang , Dezhou Xu , Li Zhang , Xiaojie Xu , Qifeng Zhu , Xiaoming Wang , Zhiqing Yang , Zehua Zhong , Jian Zhang
IPC分类号： C07C51/367 , C07C67/327 , C07D205/08 , C07C67/30 , C07C67/343 , C07C69/65 , C07C69/732 , C07C59/56
CPC分类号： C07D205/08 , C07C51/367 , C07C59/56 , C07C67/30 , C07C67/327 , C07C67/343 , C07C69/65 , C07C69/732
摘要： Disclosed is a new method for preparing an azetidinone compound represented by formula (I). The carboxylic ketoester represented by formula (II) serves as the raw material and is subjected to Grignard addition, stereoselective dehydration, ester group reduction, hydroxyl group protection, addition with imine after condensation with a chiral auxiliary, cyclization and deprotection to obtain the compound represented by formula (I). The present invention has advantages of easily available raw material, a few synthetic steps, simple operation, high yield, good stereoselectivity and low cost, and can be used for industrial production.
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公开(公告)号：US09802891B2
公开(公告)日：2017-10-31
申请号：US15386349
申请日：2016-12-21
发明人： Hongyuan Wei , Chongjun Liu , Xuyang Zhao , Xiaojie Xu , Hua Bai , Yuncai Zhang
IPC分类号： C07D205/08 , A61K31/397
CPC分类号： C07D205/08 , A61K31/397 , C07B2200/13
摘要： The present invention provides crystal forms of the compound of (3R,4S)-4-(4-hydroxyphenyl)-3-[3-(4-fluorophenyl)-4-hydroxybut-2(Z)-enyl]-1-(4-fluorophenyl)-2-azetidinone (formula A). The crystal forms can be characterized by X-ray powder diffraction (XRPD) spectra, differential scanning calorimetry (DSC) spectra, infrared absorption spectra and so on. Meanwhile, the present invention also provides methods for preparing the crystal forms of the compound of formula A, pharmaceutical compositions and uses thereof.
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公开(公告)号：US09776959B2
公开(公告)日：2017-10-03
申请号：US15386147
申请日：2016-12-21
发明人： Hongyuan Wei , Chongjun Liu , Xuyang Zhao , Xiaojie Xu , Hua Bai , Yuncai Zhang
IPC分类号： C07D205/08 , A61K31/397
CPC分类号： C07D205/08 , A61K31/397 , C07B2200/13
摘要： The present invention provides crystal forms of the compound of (3R,4S)-4-(4-hydroxyphenyl)-3-[3-(4-fluorophenyl)-4-hydroxybut-2(Z)-enyl]-1-(4-fluorophenyl)-2-azetidinone (formula A). The crystal forms can be characterized by X-ray powder diffraction (XRPD) spectra, differential scanning calorimetry (DSC) spectra, infrared absorption spectra and so on. Meanwhile, the present invention also provides methods for preparing the crystal forms of the compound of formula A, pharmaceutical compositions and uses thereof.
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公开(公告)号：US20170114016A1
公开(公告)日：2017-04-27
申请号：US15386349
申请日：2016-12-21
发明人： Hongyuan Wei , Chongjun Liu , Xuyang Zhao , Xiaojie Xu , Hua Bai , Yuncai Zhang
IPC分类号： C07D205/08
CPC分类号： C07D205/08 , A61K31/397 , C07B2200/13
摘要： The present invention provides crystal forms of the compound of (3R,4S)-4-(4-hydroxyphenyl)-3-[3-(4-fluorophenyl)-4-hydroxybut-2(Z)-enyl]-1-(4-fluorophenyl)-2-azetidinone (formula A). The crystal forms can be characterized by X-ray powder diffraction (XRPD) spectra, differential scanning calorimetry (DSC) spectra, infrared absorption spectra and so on. Meanwhile, the present invention also provides methods for preparing the crystal forms of the compound of formula A, pharmaceutical compositions and uses thereof.
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公开(公告)号：US20170114015A1
公开(公告)日：2017-04-27
申请号：US15386147
申请日：2016-12-21
发明人： Hongyuan Wei , Chongjun Liu , Xuyang Zhao , Xiaojie Xu , Hua Bai , Yuncai Zhang
IPC分类号： C07D205/08
CPC分类号： C07D205/08 , A61K31/397 , C07B2200/13
摘要： The present invention provides crystal forms of the compound of (3R,4S)-4-(4-hydroxyphenyl)-3-[3-(4-fluorophenyl)-4-hydroxybut-2(Z)-enyl]-1-(4-fluorophenyl)-2-azetidinone (formula A). The crystal forms can be characterized by X-ray powder diffraction (XRPD) spectra, differential scanning calorimetry (DSC) spectra, infrared absorption spectra and so on. Meanwhile, the present invention also provides methods for preparing the crystal forms of the compound of formula A, pharmaceutical compositions and uses thereof.
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公开(公告)号：US09567298B2
公开(公告)日：2017-02-14
申请号：US14426085
申请日：2013-09-05
发明人： Hongyuan Wei , Chongjun Liu , Xuyang Zhao , Xiaojie Xu , Hua Bai , Yuncai Zhang
IPC分类号： C07D205/08 , A61K31/397
CPC分类号： C07D205/08 , A61K31/397 , C07B2200/13
摘要： The present invention provides crystal forms of the compound of (3R,4S)-4-(4-hydroxyphenyl)-3-[3-(4-fluorophenyl)-4-hydroxybut-2(Z)-enyl]-1-(4-fluorophenyl)-2-azetidinone (formula A). The crystal forms can be characterized by X-ray powder diffraction (XRPD) spectra, differential scanning calorimetry (DSC) spectra, infrared absorption spectra and so on. Meanwhile, the present invention also provides methods for preparing the crystal forms of the compound of formula A, pharmaceutical compositions and uses thereof.
摘要翻译： 本发明提供（3R，4S）-4-（4-羟基苯基）-3- [3-（4-氟苯基）-4-羟基丁-2（Z） - 烯基] -1-（ 4-氟苯基）-2-氮杂环丁酮（式A）。 可以通过X射线粉末衍射（XRPD）光谱，差示扫描量热法（DSC）光谱，红外吸收光谱等来表征晶体形态。 同时，本发明还提供了制备式A化合物的结晶形式的方法，药物组合物及其用途。
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9.发明申请公开(公告)号：US20150218091A1
公开(公告)日：2015-08-06
申请号：US14426085
申请日：2013-09-05
发明人： Hongyuan Wei , Chongjun Liu , Xuyang Zhao , Xiaojie Xu , Hua Bai , Yuncai Zhang
IPC分类号： C07D205/08
CPC分类号： C07D205/08 , A61K31/397 , C07B2200/13
摘要： The present invention provides crystal forms of the compound of (3R,4S)-4-(4-hydroxyphenyl)-3-[3-(4-fluorophenyl)-4-hydroxybut-2(Z)-enyl]-1-(4-fluorophenyl)-2-azetidinone (formula A). The crystal forms can be characterized by X-ray powder diffraction (XRPD) spectra, differential scanning calorimetry (DSC) spectra, infrared absorption spectra and so on. Meanwhile, the present invention also provides methods for preparing the crystal forms of the compound of formula A, pharmaceutical compositions and uses thereof.
摘要翻译： 本发明提供（3R，4S）-4-（4-羟基苯基）-3- [3-（4-氟苯基）-4-羟基丁-2（Z） - 烯基] -1-（ 4-氟苯基）-2-氮杂环丁酮（式A）。 可以通过X射线粉末衍射（XRPD）光谱，差示扫描量热法（DSC）光谱，红外吸收光谱等来表征晶体形态。 同时，本发明还提供了制备式A化合物的结晶形式的方法，药物组合物及其用途。
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