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1. 发明授权

US06309881B2 Antibody catalysis of enantio- and diastereo-selective aldol reactions 有权
标题翻译：对映体和非对映选择性醛醇反应的抗体催化
公开(公告)号：US06309881B2
公开(公告)日：2001-10-30
申请号：US09824279
申请日：2001-04-02
申请人： Carlos F. Barbas , Richard A. Lerner , Guofu Zhong
发明人： Carlos F. Barbas , Richard A. Lerner , Guofu Zhong
IPC分类号： C12N512
CPC分类号： C07D417/06 , C07B2200/07 , C07D277/24 , C07D277/34 , C07D277/36 , C07D493/04 , C07K16/40 , C12N9/0002 , C12P7/26 , C12P17/16 , C12P17/18 , C12P41/002
摘要： Nine efficient aldolase antibodies were generated using hapten 2. This hapten combines, in a single molecule, structural components employed for reactive immunization with structural components employed for forming a transition state analog of the aldol reaction. Characterization of two of these antibodies reveals that they are highly proficient (up to 1000-fold better than any other antibody catalyst) and enantioselective catalysts for aldol and retro-aldol reactions and exhibit enantio- and diastereo-selectivities opposite that of antibody 38C2.
摘要翻译：使用半抗原2产生九种有效的醛缩酶抗体。该半抗原在单个分子中结合用于反应性免疫的结构组分与用于形成醛醇反应的过渡态类似物的结构组分。这些抗体中的两种的表征显示它们是非常熟练的（比任何其他抗体催化剂优于1000倍）和对映体选择性催化剂，用于醛醇醛和醛缩醇反应，并显示与抗体38C2相反的对映体和非对映体选择性。

2. 发明授权

US07666658B1 Antibody catalysis of enantio- and diastereo-selective aldol reactions 有权
标题翻译：对映体和非对映选择性醛醇反应的抗体催化
公开(公告)号：US07666658B1
公开(公告)日：2010-02-23
申请号：US10110181
申请日：2000-10-06
申请人： Carlos F. Barbas , Richard A. Lerner , Guofu Zhong
发明人： Carlos F. Barbas , Richard A. Lerner , Guofu Zhong
IPC分类号： C12S13/00 , C12N9/00 , C12P7/26
CPC分类号： C07D277/24 , C07B57/00 , C07B2200/07 , C07D277/34 , C07D277/36 , C07D417/06 , C07D493/04 , C12N9/0002 , C12P7/26 , C12P13/02 , C12P41/00 , C12P41/002
摘要： Nine efficient aldolase antibodies were generated using hapten 2. This hapten combines, in a single molecule, structural components employed for reactive immunization with structural components employed for forming a transition state analog of the aldol reaction. Characterization of two of these antibodies reveals that they are highly proficient (up to 1000-fold better than any other antibody catalyst) and enantioselective catalysts for aldol and retro-aldol reactions and exhibit enantio- and diastereo-selectivities opposite that of antibody 38C2.
摘要翻译：使用半抗原2产生九种有效的醛缩酶抗体。该半抗原在单个分子中结合用于反应性免疫的结构组分与用于形成醛醇反应的过渡态类似物的结构组分。这些抗体中的两种的表征显示它们是非常熟练的（比任何其他抗体催化剂优于1000倍）和对映体选择性催化剂，用于醛醇醛和醛缩醇反应，并显示与抗体38C2相反的对映体和非对映体选择性。

3. 发明授权

US06589766B1 Aldol consensations by catalytic antibodies 失效
标题翻译：通过催化抗体的Aldol认可
公开(公告)号：US06589766B1
公开(公告)日：2003-07-08
申请号：US09965512
申请日：2001-09-25
申请人： Carlos F. Barbas , Richard A. Lerner , Guofu Zhong , Benjamin List
发明人： Carlos F. Barbas , Richard A. Lerner , Guofu Zhong , Benjamin List
IPC分类号： C12P726
CPC分类号： C12P7/26 , C12N9/0002
摘要： Catalytic antibodies, including 38C2 and 33F12, are capable of efficiently catalyzing a wide variety of ketone-ketone, ketone-aldehyde, aldehyde-ketone, and aldehyde-aldehyde intermolecular aldol reactions, and in some cases to catalyze their subsequent dehydration to yield aldol condensation products. A number of intramolecular aldol reactions have also been defined. Catalysis of all intramolecular aldol reactions examined yields the corresponding condensation products.
摘要翻译：包括38C2和33F12在内的催化抗体能够有效地催化各种酮 - 酮，酮 - 醛，醛 - 酮和醛 - 醛分子间醛醇反应，并且在某些情况下催化它们随后的脱水以产生醛醇缩合产品。还定义了许多分子内醛醇反应。所检测的所有分子内醛醇反应的催化产生相应的缩合产物。

4. 发明授权

US06326176B1 Aldol condensations by catalytic antibodies 失效
标题翻译：通过催化抗体的醛醇缩合
公开(公告)号：US06326176B1
公开(公告)日：2001-12-04
申请号：US09573753
申请日：2000-05-18
申请人： Carlos F. Barbas , Richard A. Lerner , Guofu Zhong , Benjamin List
发明人： Carlos F. Barbas , Richard A. Lerner , Guofu Zhong , Benjamin List
IPC分类号： C12P726
CPC分类号： C12P7/26 , C12N9/0002
摘要： Catalytic antibodies, including 38C2 and 33F12, are capable of efficiently catalyzing a wide variety of ketone-ketone, ketone-aldehyde, aldehyde-ketone, and aldehyde-aldehyde intermolecular aldol reactions, and in some cases to catalyze their subsequent dehydration to yield aldol condensation products. A number of intramolecular aldol reactions have also been defined. Catalysis of all intramolecular aldol reactions examined yields the corresponding condensation products.
摘要翻译：包括38C2和33F12在内的催化抗体能够有效地催化各种酮 - 酮，酮 - 醛，醛 - 酮和醛 - 醛分子间醛醇反应，并且在某些情况下催化它们随后的脱水以产生醛醇缩合产品。还定义了许多分子内醛醇反应。所检测的所有分子内醛醇反应的催化产生相应的缩合产物。

5. 发明授权

US06210938B1 Antibody catalysis of enantio- and diastereo-selective aldol reactions 有权
标题翻译：对映体和非对映选择性醛醇反应的抗体催化
公开(公告)号：US06210938B1
公开(公告)日：2001-04-03
申请号：US09458367
申请日：1999-12-09
申请人： Carlos F. Barbas , Richard A. Lerner , Guofu Zhong
发明人： Carlos F. Barbas , Richard A. Lerner , Guofu Zhong
IPC分类号： C12P726
CPC分类号： C07D417/06 , C07B2200/07 , C07D277/24 , C07D277/34 , C07D277/36 , C07D493/04 , C12N9/0002 , C12P7/26 , C12P17/16 , C12P17/18 , C12P41/002
摘要： Nine efficient aldolase antibodies were generated using hapten 2. This hapten combines, in a single molecule, structural components employed for reactive immunization with structural components employed for forming a transition state analog of the aldol reaction. Characterization of two of these antibodies reveals that they are highly proficient (up to 1000-fold better than any other antibody catalyst) and enantioselective catalysts for aldol and retro-aldol reactions and exhibit enantio- and diastereo- selectivities opposite that of antibody 38C2.
摘要翻译：使用半抗原2产生九种有效的醛缩酶抗体。该半抗原在单个分子中结合用于反应性免疫的结构组分与用于形成醛醇反应的过渡态类似物的结构组分。这些抗体中的两种的表征显示它们是非常熟练的（比任何其他抗体催化剂优于1000倍）和用于醛醇醛和醛缩醇反应的对映选择性催化剂，并显示与抗体38C2相反的对映体和非对映体选择性。

6. 发明授权

US08273901B2 Process of forming a pyrrole compound 有权
标题翻译：形成吡咯化合物的方法
公开(公告)号：US08273901B2
公开(公告)日：2012-09-25
申请号：US12782708
申请日：2010-05-18
申请人： Guofu Zhong , Bin Tan , Zugui Shi , Pei Juan Chua
发明人： Guofu Zhong , Bin Tan , Zugui Shi , Pei Juan Chua
IPC分类号： C07D207/30
CPC分类号： C07D207/46
摘要： Disclosed is a process of forming a pyrrole compound. The process comprises contacting an α-carbonyl oxime compound 1 and an α,β-unsaturated aldehyde 2 R1 and R2 in compound 1 are independently selected from the group consisting of H, a silyl-group, an aliphatic group, an alicyclic group, an aromatic group, an arylaliphatic group, and an arylalicyclic group. The aliphatic, alicyclic, aromatic, arylaliphatic, and arylalicyclic groups comprise 0 to about 3 heteroatoms selected from the group N, O, S, Se and Si. R3 in aldehyde 2 is selected from the group consisting of H, a silyl-group, an aliphatic group, an alicyclic group, an aromatic group, an arylaliphatic group, and an arylalicyclic group. The aliphatic, alicyclic, aromatic, arylaliphatic, and arylalicyclic groups comprise 0 to about 3 heteroatoms selected from the group N, O, S, Se and Si. The α-carbonyl oxime compound 1 an the α,β-unsaturated aldehyde 2 are contacted in a suitable solvent in the presence of a secondary amine. The compounds are contacted for a sufficient period of time to allow the formation of an N-hydroxypyrrole compound 3
摘要翻译：公开了形成吡咯化合物的方法。该方法包括使α-羰基肟化合物1和化合物1中的α，bgr-不饱和醛2 R1和R2独立地选自H，甲硅烷基，脂族基，脂环基，芳基，芳基脂族基和芳基脂环基。脂族，脂环族，芳族，芳基脂族和芳基脂环基包含0至约3个选自N，O，S，Se和Si的杂原子。醛2中的R 3选自H，甲硅烷基，脂族基，脂环族基，芳族基，芳基脂族基和芳基脂环基。脂族，脂环族，芳族，芳基脂族和芳基脂环基包含0至约3个选自N，O，S，Se和Si的杂原子。 α-羰基肟化合物1和α，bgr-不饱和醛2在适当的溶剂中，在仲胺的存在下接触。使化合物接触足够的时间以允许形成N-羟基吡咯化合物3

7. 发明授权

US08940938B2 Michael reaction with recovery of the catalyst 有权
标题翻译：迈克尔反应与催化剂的回收
公开(公告)号：US08940938B2
公开(公告)日：2015-01-27
申请号：US12782706
申请日：2010-05-18
申请人： Guofu Zhong , Bin Tan , Xuan Zhang , Pei Juan Chua
发明人： Guofu Zhong , Bin Tan , Xuan Zhang , Pei Juan Chua
IPC分类号： C07C205/03 , C07D333/22 , C07C201/12 , C07D307/46 , C07D401/06
CPC分类号： C07D333/22 , C07C201/12 , C07D307/46 , C07D401/06 , C07C205/45
摘要： Disclosed is a process of carrying out a Michael reaction with recovery of the catalyst, where a compound of formula (1): is reacted with a compound of formula (2): in the presence of a catalyst of formula (4): where the compounds of formulae (1) and (2) undergo a Michael reaction.
摘要翻译：公开了在式（4）的催化剂存在下，使式式（1）和（2）的化合物经历迈克尔反应。

8. 发明授权

US08754252B2 Asymmetric cyclization processes using unsaturated nitro compounds 有权
标题翻译：使用不饱和硝基化合物的不对称环化过程
公开(公告)号：US08754252B2
公开(公告)日：2014-06-17
申请号：US13541648
申请日：2012-07-03
申请人： Guofu Zhong , Bin Tan , Pei Juan Chua , Zugui Shi
发明人： Guofu Zhong , Bin Tan , Pei Juan Chua , Zugui Shi
IPC分类号： C07C201/12
CPC分类号： C07C201/12 , C07C2601/08 , C07C2601/14 , C07D307/54 , C07D333/24 , C07C205/55
摘要： Disclosed are processes of forming a compound (33), (35) or (37)
摘要翻译：公开了形成化合物（33），（35）或（37）的方法，

9. 发明申请

US20110124881A1 PROCESS OF FORMING A PYRROLE COMPOUND 有权
标题翻译：形成吡咯烷酮化合物的方法
公开(公告)号：US20110124881A1
公开(公告)日：2011-05-26
申请号：US12782708
申请日：2010-05-18
申请人： Guofu Zhong , Bin Tan , Zugui Shi , Pei Juan Chua
发明人： Guofu Zhong , Bin Tan , Zugui Shi , Pei Juan Chua
IPC分类号： C07D207/46
CPC分类号： C07D207/46
摘要： Disclosed is a process of forming a pyrrole compound. The process comprises contacting an α-carbonyl oxime compound 1 and an α,β-unsaturated aldehyde 2 R1 and R2 in compound 1 are independently selected from the group consisting of H, a silyl-group, an aliphatic group, an alicyclic group, an aromatic group, an arylaliphatic group, and an arylalicyclic group. The aliphatic, alicyclic, aromatic, arylaliphatic, and arylalicyclic groups comprise 0 to about 3 heteroatoms selected from the group N, O, S, Se and Si. R3 in aldehyde 2 is selected from the group consisting of H, a silyl-group, an aliphatic group, an alicyclic group, an aromatic group, an arylaliphatic group, and an arylalicyclic group. The aliphatic, alicyclic, aromatic, arylaliphatic, and arylalicyclic groups comprise 0 to about 3 heteroatoms selected from the group N, O, S, Se and Si. The α-carbonyl oxime compound 1 an the α,β-unsaturated aldehyde 2 are contacted in a suitable solvent in the presence of a secondary amine. The compounds are contacted for a sufficient period of time to allow the formation of an N-hydroxypyrrole compound 3
摘要翻译：公开了形成吡咯化合物的方法。该方法包括使α-羰基肟化合物1和化合物1中的α，bgr-不饱和醛2 R1和R2独立地选自H，甲硅烷基，脂族基，脂环基，芳基，芳基脂族基和芳基脂环基。脂族，脂环族，芳族，芳基脂族和芳基脂环基包含0至约3个选自N，O，S，Se和Si的杂原子。醛2中的R 3选自H，甲硅烷基，脂族基，脂环族基，芳族基，芳基脂族基和芳基脂环基。脂族，脂环族，芳族，芳基脂族和芳基脂环基包含0至约3个选自N，O，S，Se和Si的杂原子。 α-羰基肟化合物1和α，bgr-不饱和醛2在适当的溶剂中，在仲胺的存在下接触。使化合物接触足够的时间以允许形成N-羟基吡咯化合物3

10. 发明授权

US08680335B2 Processes of enantioselectively forming an aminoxy compound and an 1,2-oxazine compound 有权
标题翻译：对映选择性形成氨氧基化合物和1,2-恶嗪化合物的方法
公开(公告)号：US08680335B2
公开(公告)日：2014-03-25
申请号：US12782709
申请日：2010-05-18
申请人： Guofu Zhong , Min Lu , Di Zhu , Pei Juan Chua , Bin Tan
发明人： Guofu Zhong , Min Lu , Di Zhu , Pei Juan Chua , Bin Tan
IPC分类号： C07C209/38 , C07D265/02
CPC分类号： C07D265/02 , C07C239/20
摘要： Disclosed is a process of enantioselectively forming an aminoxy compound of Formula (3) In formula (3) R1 is one of an aliphatic group and an alicyclic group. R2 is one of hydrogen, an aliphatic group, an alicyclic group, an aromatic group, an arylaliphatic group and an arylalicyclic group. R3 is one of hydrogen, halogen, hydroxyl, and an aliphatic group with a main chain having 1 to about 10 carbon atoms. The respective aliphatic, alicyclic, aromatic, arylaliphatic or arylalicyclic groups of R1, R2, and R3 comprise 0 to about 3 heteroatoms independently selected from the group consisting of N, O, S, Se and Si. The process includes contacting a carbonyl compound of Formula (1) and a nitroso compound of Formula (2) in the presence of a chiral catalyst. The chiral catalyst is a compound of Formula (IX)
摘要翻译：公开了对映选择性地形成式（3）的氨氧基化合物的方法。在式（3）中，R 1是脂族基和脂环基之一。 R2是氢，脂肪族基团，脂环族基团，芳香族基团，芳基脂族基团和芳基脂环族基团中的一种。 R 3是氢，卤素，羟基和具有1至约10个碳原子的主链的脂族基团之一。 R 1，R 2和R 3各自的脂族，脂环族，芳族，芳基脂族或芳基脂环基包含0至约3个独立地选自N，O，S，Se和Si的杂原子。该方法包括在手性催化剂的存在下使式（1）的羰基化合物与式（2）的亚硝基化合物接触。手性催化剂是式（IX）的化合物，

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