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1.发明申请公开(公告)号：US20120330015A1
公开(公告)日：2012-12-27
申请号：US13581173
申请日：2010-09-16
申请人： Eelco Ruijter , Romano Orru , Anass Znabet , Marloes Polak , Nicholas Turner
发明人： Eelco Ruijter , Romano Orru , Anass Znabet , Marloes Polak , Nicholas Turner
IPC分类号： C07C231/14 , C07C265/04 , C07C237/22 , C07C263/00 , C07D403/12
CPC分类号： C07C291/10 , C07C231/06 , C07C237/14 , C07C2601/02 , C07C2601/04 , C07D209/52 , C07D209/58 , C07D209/94 , C07D241/24 , C07D403/06 , C07D403/12
摘要： The present invention relates to a process for the preparation of a compound of the general Formula (I), comprising: a) reacting a compound of the general Formula (II) with a compound of the Formula III R2COOH and a compound of the general Formula IV R3NC under such conditions that compound I is formed, wherein R1 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R2 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R3 represents a substituted or unsubstituted alkyl, alkenyl, or alkynyl structure. In further aspect the subject invention relates to the use of the obtained products as intermediates for various peptidomimetics, and preferably as a building block in a convergent synthesis of prolyl dipeptide structures.
摘要翻译： 本发明涉及制备通式（I）化合物的方法，包括：a）使通式（II）的化合物与式III的化合物R 2 COOH和通式 IV R3NC在这样的条件下形成化合物I，其中R 1表示取代或未取代的烷基，烯基，炔基，芳族或非芳族，单 - ，二 - 或三环或杂环结构，并且R 2表示取代或未取代的烷基 烯基，炔基，芳族或非芳族，单 - ，二 - 或三环或杂环结构，并且R 3表示取代或未取代的烷基，烯基或炔基结构。 在另一方面，本发明涉及所得产物作为各种肽模拟物的中间体的用途，优选作为脯氨酰二肽结构的会聚合成中的结构单元。
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公开(公告)号：US08686145B2
公开(公告)日：2014-04-01
申请号：US13581173
申请日：2010-09-16
申请人： Eelco Ruijter , Romano Orru , Anass Znabet , Marloes Polak , Nicholas Turner
发明人： Eelco Ruijter , Romano Orru , Anass Znabet , Marloes Polak , Nicholas Turner
IPC分类号： C07C291/10 , C07D209/52 , C07D209/58 , C07D209/94 , C07D241/24 , C07D403/06
CPC分类号： C07C291/10 , C07C231/06 , C07C237/14 , C07C2601/02 , C07C2601/04 , C07D209/52 , C07D209/58 , C07D209/94 , C07D241/24 , C07D403/06 , C07D403/12
摘要： The present invention relates to a process for the preparation of a compound of the general Formula (I), comprising: a) reacting a compound of the general Formula (II) with a compound of the Formula III R2COOH and a compound of the general Formula IV R3NC under such conditions that compound I is formed, wherein R1 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R2 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R3 represents a substituted or unsubstituted alkyl, alkenyl, or alkynyl structure. In further aspect the subject invention relates to the use of the obtained products as intermediates for various peptidomimetics, and preferably as a building block in a convergent synthesis of prolyl dipeptide structures.
摘要翻译： 本发明涉及制备通式（I）化合物的方法，包括：a）使通式（II）的化合物与式III的化合物R 2 COOH和通式 IV R3NC在这样的条件下形成化合物I，其中R 1表示取代或未取代的烷基，烯基，炔基，芳族或非芳族，单 - ，二 - 或三环或杂环结构，并且R 2表示取代或未取代的烷基 烯基，炔基，芳族或非芳族，单 - ，二 - 或三环或杂环结构，并且R 3表示取代或未取代的烷基，烯基或炔基结构。 在另一方面，本发明涉及所得产物作为各种肽模拟物的中间体的用途，优选作为脯氨酰二肽结构的会聚合成中的结构单元。
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3.发明申请PROCESS FOR THE PREPARATION OF SUBSTITUTED PROLYL PEPTIDES AND SIMILAR PEPTIDOMIMETICS 审中-公开制备替代的丙型肝炎肽和类似物的方法公开(公告)号：US20120329704A1
公开(公告)日：2012-12-27
申请号：US13581179
申请日：2010-09-16
申请人： Eelco Ruijter , Romano Orru , Anass Znabet , Marloes Polak , Nicholas Turner
发明人： Eelco Ruijter , Romano Orru , Anass Znabet , Marloes Polak , Nicholas Turner
CPC分类号： C07C291/10 , C07C231/06 , C07C237/14 , C07C2601/02 , C07C2601/04 , C07D209/52 , C07D209/58 , C07D209/94 , C07D241/24 , C07D403/06 , C07D403/12
摘要： The present invention relates to a process for the stereoselective preparation of a compound having the general formula (I) or its respective diastereomers: comprising reacting a compound having the general formula (II) or its diastereomers: with a compound of the general formula III: R3—COOH and a compound of the general formula IV: R4—NC wherein R1 represents each independently, or jointly a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R2 represents a hydrogen atom, a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R3 represents a substituted or unsubstituted alkyl, alkenyl, or alkynyl, or an aromatic or non-aromatic aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure. R3—COOH (III) R4—NC (IV)
摘要翻译： 本发明涉及具有通式（I）或其相应非对映异构体的立体选择性制备方法：包括使具有通式（II）的化合物或其非对映体与通式III的化合物反应： R3-COOH和通式IV的化合物：R4-NC，其中R1各自独立地表示，或者共同取代或未取代的烷基，烯基，炔基，芳族或非芳族，单 - ，二 - 或三环或杂环结构 ，R 2表示氢原子，取代或未取代的烷基，烯基，炔基，芳族或非芳香族，单 - ，二 - 或三环或杂环结构，R 3表示取代或未取代的烷基，烯基或炔基， 或芳族或非芳族芳族或非芳族，单 - ，二 - 或三环或杂环结构。 R3-COOH（III）R4-NC（IV）
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