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1. 发明申请

US20060069283A1 New process 审中-公开
标题翻译：新进程
公开(公告)号：US20060069283A1
公开(公告)日：2006-03-30
申请号：US11282247
申请日：2005-11-18
申请人： Kjell Andersson , Alan Fischer , Panagiotis Ioannidis , Magnus Larsson , Maria Larsson , Sivaprasad Sivadasan
发明人： Kjell Andersson , Alan Fischer , Panagiotis Ioannidis , Magnus Larsson , Maria Larsson , Sivaprasad Sivadasan
IPC分类号： C07C69/76
CPC分类号： C07C69/734 , C07B2200/07 , C07C51/377 , C07C51/412 , C07C59/64
摘要： The present invention relates to novel resolution methods, which are useful in the preparation of enantiomerically enriched intermediates which in their turn are useful in the prepartion of compounds with a pharmacological effect on the insulin resistance syndrome (IRS). It is such a process that the present inventions sets out to define, and more particularly for the preparation of the (S)-enantioner of certain 2-ethoxy-3-(4-hydroxyphenyl)propanoic acids and derivatives thereof.
摘要翻译：本发明涉及新的拆分方法，其可用于制备对映异构体富集的中间体，其可用于制备对胰岛素抵抗综合征（IRS）具有药理作用的化合物。正是这样一个过程，本发明规定了，特别是制备某些2-乙氧基-3-（4-羟基苯基）丙酸及其衍生物的（S） - 连接剂。

2. 发明授权

US07002037B2 Process for the preparation on enantiomerically enriched compounds 失效
标题翻译：制备富含对映异构体的化合物的方法
公开(公告)号：US07002037B2
公开(公告)日：2006-02-21
申请号：US10148818
申请日：2000-11-29
申请人： Kjell Andersson , Alan Eric Fischer , Panagiotis Ioannidis , Magnus Larsson , Maria Larsson , Sivaprasad Sivadasan
发明人： Kjell Andersson , Alan Eric Fischer , Panagiotis Ioannidis , Magnus Larsson , Maria Larsson , Sivaprasad Sivadasan
IPC分类号： C07C261/00 , C07C59/48
CPC分类号： C07C69/734 , C07B2200/07 , C07C51/377 , C07C51/412 , C07C59/64
摘要： The present invention relates to novel resolution methods, which are useful in the preparation of enantiomerically enriched intermediates which in their turn are useful in the prepartion of compounds with a pharmacological effect on the insulin resistance syndrome (IRS). It is such a process that the present inventions sets out to define, and more particularly for the preparation of the (S)-enantioner of certain 2-ethoxy-3-(4-hydroxyphenyl)propanoic acids and derivatives thereof.
摘要翻译：本发明涉及新的拆分方法，其可用于制备对映异构体富集的中间体，其可用于制备对胰岛素抵抗综合征（IRS）具有药理作用的化合物。正是这样一个过程，本发明规定了，特别是制备某些2-乙氧基-3-（4-羟基苯基）丙酸及其衍生物的（S） - 连接剂。

3. 发明申请

US20080319206A1 Process for Preparing Protected Amidines 审中-公开
标题翻译：制备保护脒的方法
公开(公告)号：US20080319206A1
公开(公告)日：2008-12-25
申请号：US11816998
申请日：2006-02-22
申请人： Firas Al-Saffar , Stefan Berlin , Tibor Musil , Sivaprasad Sivadasan
发明人： Firas Al-Saffar , Stefan Berlin , Tibor Musil , Sivaprasad Sivadasan
IPC分类号： C07D205/04 , C07C257/10
CPC分类号： C07C259/14 , C07C259/18 , C07D205/04 , C07D209/18
摘要： A process for preparing a protected amidine group of formula (I): wherein R6 represents, for example, C1-10 alkyl (optionally substituted), aryl, C1-3 alkylaryl or C1-3 alkyloxyaryl; which comprises reacting a nitrile containing compound with an oxyamine of formula (II): R6ONH2 wherein R6 is as defined above for (I); in the presence of a thio-keto activating agent of formula (III): HS—Ry, —C(O)-Z wherein Z is -(1-4C)alkyl, —OH, —O-(1-4C)alkyl, —SH, —S(1-4C)alkyl, —NH2, —NH(1-4C)alkyl or —N[(1-4C)alkyl]2; Ry is (1-2C)alkyl (optionally substituted); or Z and Ry are linked so as to form a 5- or 6-membered ring of formula (IV): wherein X is —CH2—, —O—, —NH— or —N(1-4C)alkyl; p is 1 or 2; m is 1 or 2 and Rz is independently selected from H, (1-4C)alkyl, halo and amino.
摘要翻译：制备式（I）的保护的脒基的方法：其中R 6表示例如C 1-10烷基（任选取代的），芳基，C 1-3烷基芳基或C 1-3烷氧基芳基; 其包括使含腈化合物与式（II）的氧胺反应：R6ONH2，其中R6如对于（I）所定义; 在式（III）的硫代酮活化剂存在下：HS-Ry，-C（O）-Z其中Z是 - （1-4C）烷基，-OH，-O-（1-4C）烷基，-SH，-S（1-4C）烷基，-NH 2，-NH（1-4C）烷基或-N [（1-4C）烷基] 2; Ry是（1-2C）烷基（任选取代的）; 或Z和Ry连接形成式（Ⅳ）的5-或6-元环：其中X是-CH 2 - ， - O - ， - NH-或-N（1-4C）烷基; p为1或2; m为1或2，Rz独立地选自H，（1-4C）烷基，卤素和氨基。

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