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公开(公告)号:US20030040644A1
公开(公告)日:2003-02-27
申请号:US10190105
申请日:2002-07-03
发明人: Richard L. Gabriel , Adel M. Moussa , Sharon Fitzhenry , Changhua Liu , David A. Swanson , Brittany Le , Salah Zahr , Yesh P. Sachdeva , Jurjus Jurayj
IPC分类号: C07D233/61 , C07D209/16 , C07D207/46 , C07C29/78
CPC分类号: C07C213/00 , C07B2200/07 , Y02P20/55 , C07C215/08
摘要: The present invention relates to a method of preparing a 1-nitro-3-substituted-3-amino-2-propanol diastereomer represented by Structural Formula I: 1 In Structural Formula I, R is an amine protecting group, and R1 is an amino acid side-chain, a protected amino acid side-chain, a substituted or unsubstituted aliphatic group, a substituted or unsubstituted aromatic group, a substituted or unsubstituted heteroaromatic group, a substituted or unsubstituted aralkyl or a substituted or unsubstituted heteroaralkyl group. The method involves contacting a 1-nitro-3-substituted-3-amino-2-propanone with a reducing agent to form a mixture of 1-nitro-3-substituted-3-amino-2-propanol diastereomers. The 1-nitro-3-substituted-3-amino-2-propanol diastereomers are then separated by simulated moving bed chromatography to obtain one or more 1-nitro-3-substituted-3-amino-2-propanol diastereomer.
摘要翻译: 本发明涉及由结构式I表示的1-硝基-3-取代-3-氨基-2-丙醇非对映体的制备方法:在结构式I中,R是胺保护基,R 1是氨基酸 取代或未取代的芳族基团,取代或未取代的杂芳族基团,取代或未取代的芳烷基或取代或未取代的杂芳烷基。 该方法包括使1-硝基-3-取代-3-氨基-2-丙酮与还原剂接触以形成1-硝基-3-取代-3-氨基-2-丙醇非对映异构体的混合物。 然后通过模拟移动床层析分离1-硝基-3-取代-3-氨基-2-丙醇非对映异构体,得到一种或多种1-硝基-3-取代-3-氨基-2-丙醇非对映异构体。
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公开(公告)号:US20020188135A1
公开(公告)日:2002-12-12
申请号:US10178180
申请日:2002-06-21
发明人: Richard L. Gabriel , Jurjus Jurayj
IPC分类号: C07D233/61
CPC分类号: C07C291/10 , C07C211/13 , C40B40/00 , Y02P20/55
摘要: Disclosed are novel compounds represented by Structural Formula II, IX or XXVIII: 1 R1, R2, and R22 are independently an aliphatic group, a substituted aliphatic group, an aromatic group or a substituted aromatic group. R2 is nullNR4R5 or nullNnullnullCnull. Alternatively, R1, and R2, taken together with the methine group to which they are bonded, are a moiety represented by the following structural formula: 2 R3 is nullNH2, nullOH, nullOC(O)H or nullOR9. R5, R6 and R7 are independently nullH or an amine protecting group. R8 is nullH, nullOH or nullOR8. R9 is an alcohol protecting group. Also disclosed are methods of preparing these compounds.
摘要翻译: 公开了由结构式II,IX或XXVIII表示的新化合物:R1,R2和R22独立地是脂族基团,取代的脂族基团,芳族基团或取代的芳族基团。 R2是-NR4R5或-N + = C-。 或者,R 1和R 2与它们所键合的次甲基一起是由以下结构式表示的部分:R 3是-NH 2,-OH,-OC(O)H或-OR 9。 R5,R6和R7独立地为-H或胺保护基。 R8是-H,-OH或-OR8。 R9是醇保护基。 还公开了制备这些化合物的方法。
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