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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：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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