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1. 发明授权

US07256259B2 Methods for ligation of molecules to surfaces 有权
标题翻译：将分子连接到表面的方法
公开(公告)号：US07256259B2
公开(公告)日：2007-08-14
申请号：US10930702
申请日：2004-08-30
申请人： Ronald T. Raines , Matthew B. Soellner
发明人： Ronald T. Raines , Matthew B. Soellner
IPC分类号： B05D3/10 , C07K1/04 , C07K17/00 , C23C22/00 , H01L21/02
CPC分类号： C07K1/1077 , C07F9/4866 , C07F9/5004 , C07F9/5022 , C07F9/5054 , C07K1/082 , C07K1/1072 , Y10S530/81
摘要： The present invention is a method for a covalent ligation of one or more molecules to one or more surfaces, that is site-specific and both rapid and high yielding. The covalent ligation to the surface is based on the reaction of an azide and a phosphinothioester to form an amide bond. The method of the invention is particularly well-suited to the immobilization of peptides, proteins or protein fragments to surfaces.
摘要翻译：本发明是一种或多种分子与一个或多个表面共价连接的方法，其是位点特异性的并且快速和高产率。与表面的共价连接基于叠氮化物和膦硫代酯的反应以形成酰胺键。本发明的方法特别适用于将肽，蛋白质或蛋白质片段固定在表面上。

2. 发明申请

US20040087779A1 Ligation method and reagents to form an amide bond 有权
标题翻译：连接方法和试剂形成酰胺键
公开(公告)号：US20040087779A1
公开(公告)日：2004-05-06
申请号：US10276515
申请日：2003-01-23
发明人： Ronald T. Raines , Laura L. Kiessling , Bradley L. Nilsson
IPC分类号： C07K001/04 , C07F009/28
CPC分类号： C07K1/082 , C07F9/4866 , C07F9/5004 , C07F9/5022 , C07F9/5054 , C07K1/1072 , C07K1/1077
摘要： Methods and reagents for the formation of amide bonds between an activated carboxylic acid derivative and an azide useful in the synthesis of peptides, proteins and derivatized or labeled amino acids, peptide or proteins. The method involves the formation of a phosphinothioester which reacts with an azide resulting in amide formation. The invention provides phosphinothiol reagents which convert activated carboxylic acid derivatives to phosphinothioesters which then react with azides to form an amide bond. The methods and reagents of the invention can be used for stepwise synthesis of peptides on solid supports or for the ligation to two or more amino acids, two or more peptide or two or more protein fragments.
摘要翻译：用于在合成肽，蛋白质和衍生化或标记的氨基酸，肽或蛋白质中有用的活化的羧酸衍生物和叠氮化物之间形成酰胺键的方法和试剂。该方法涉及形成与产生酰胺形成的叠氮化物反应的膦硫代酯。本发明提供了将活化的羧酸衍生物转化为硫代磷酸酯的次硫基硫醇试剂，然后与叠氮化物反应形成酰胺键。本发明的方法和试剂可用于在固体支持物上逐步合成肽或用于连接至两个或更多个氨基酸，两个或更多个肽或两个或更多个蛋白质片段。

3. 发明授权

US06222032B1 Use of ylides of phosphorus as slightly nuceophilic strong bases 失效
标题翻译：使用磷酸内鎓盐作为微乳液的强碱
公开(公告)号：US06222032B1
公开(公告)日：2001-04-24
申请号：US09423269
申请日：1999-11-04
申请人： Guy Bertrand , Dennis Bigg , Jean-Bernard Cazaux , Stéphanie Goumri , Olivier Guerret
发明人： Guy Bertrand , Dennis Bigg , Jean-Bernard Cazaux , Stéphanie Goumri , Olivier Guerret
IPC分类号： C07D24316
CPC分类号： C07D207/267 , C07D227/087 , C07D243/16 , C07F9/5352 , C07K1/082 , C08F8/40
摘要： In a process for C-alkylation or N-alkylation, the improvement comprising conducting the C-alkylation or N-alkylation reaction in the presence of a slightly nucleophilic strong base of the following formula wherein R′1, R′2 and R′3 are individually selected from the group consisting of alkoxy of 1 to 6 carbon atoms and R′ and R″ are individually selected from the group consisting of unsubstituted or substituted alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, aryl and aralkyl of 1 to 6 alkyl carbon atoms, the substituents being selected from the group consisting of halogen, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, —CN, —NO2 and dialkylamino of 1 to 6 alkyl carbon atoms, the aryl being selected from the group consisting of unsaturated monocyclic and condensed carbocyclic and heterocyclic with at least one heteroatom selected from the group consisting of nitrogen, oxygen and sulfur, R′4 is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and alkoxy of 1 to 6 carbon atoms and R′5 is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms and a polymeric support.
摘要翻译：在C-烷基化或N-烷基化方法中，包括在R'1，R'2和R'3的下列化学式的轻微亲核强碱存在下进行C-烷基化或N-烷基化反应的改进是分别选自1至6个碳原子的烷氧基和R'和R“分别选自未取代或取代的1至6个碳原子的烷基，1至6个碳原子的烷氧基，3个环烷基至10个碳原子，芳基和1至6个烷基碳原子的芳烷基，取代基选自卤素，1至6个碳原子的烷基，1至6个碳原子的烷氧基，-CN，-NO 2和二烷基氨基 1至6个烷基碳原子，芳基选自不饱和单环和稠合的碳环和杂环与至少一个选自氮，氧和硫的杂原子，R '4选自组氢，1至6个碳原子的烷基和1至6个碳原子的烷氧基和R'5选自氢，1至6个碳原子的烷基，1至6个碳原子的烷氧基和聚合物支持。

4. 发明授权

US4173563A Phosphonium salt and its use 失效
标题翻译：鏻盐及其用途
公开(公告)号：US4173563A
公开(公告)日：1979-11-06
申请号：US914773
申请日：1978-06-12
申请人： Noboru Yamazaki , Fukuji Higashi
发明人： Noboru Yamazaki , Fukuji Higashi
IPC分类号： C07D209/20 , C07C67/00 , C07C231/00 , C07K1/06 , C07K1/08 , C07K1/10 , C07K5/06 , C07C103/52 , C07G7/00
CPC分类号： C07K1/08 , C07K1/082 , C07K5/06026
摘要： The amidation and esterification of carboxylic acids with amines and hydroxyl group-containing compounds, respectively, are effected without incurring the drawbacks of reaction equilibrium by the reaction of the reactants, one of which has been activated in the reactive group by contact with a phosphonium salt obtained by reacting a phosphorous ester or phosphorous monoester salt with an organic base such as pyridine and an oxidizing agent such as halogens and mono or divalent mercury halide or acetate. The amidation can be applied to the preparation of peptides by the reaction of amino acids and/or peptides in which one of the reactive groups have been protected.
摘要翻译：羧酸与胺和含羟基化合物的酰胺化和酯化反应分别在不引起反应平衡的缺点的情况下进行，反应物的反应已经通过与鏻盐的接触活化在反应性基团中通过使磷酯或磷单酯盐与有机碱如吡啶和氧化剂如卤素和一价或二价卤化汞或乙酸酯反应而获得。酰胺化可以通过其中一个反应性基团被保护的氨基酸和/或肽的反应应用于肽的制备。

5. 发明授权

US3737423A Process for the preparation of a carboxylic acid amide 失效
标题翻译：制备羧酸酰胺的方法
公开(公告)号：US3737423A
公开(公告)日：1973-06-05
申请号：US3737423D
申请日：1970-11-17
申请人： SANKYO CO
发明人： MUKAIYAMA T , UEKI M , MATSUEDA R , MARUYAMA H
IPC分类号： B01J31/00 , C07B31/00 , C07B43/06 , C07B61/00 , C07C67/00 , C07C231/00 , C07C231/02 , C07C313/00 , C07C319/20 , C07C323/60 , C07D499/00 , C07D499/12 , C07K1/08 , C07K1/10 , C07K5/065 , C07C103/52 , C07G7/00
CPC分类号： C07K1/086 , C07D499/00 , C07K1/082 , C07K1/084 , C07K5/06078
摘要： AN IMPROVED AND NOVEL PROCESS FOR THE PREPARATION OF A CARBOXYLIC ACID AMIDE WHICH COMPRISES REACTING A CARBOXYLIC ACID WITH AN ORGANIC AMINE OR A SULFENIC ACID WITH AN ORGANIC AMINE OR A SULFENIC ACID AMIDE THEREOF IN THE PRESENCE OF A TERTIARY PHOSPHINE AND A DISULFIDE OF A MERCAPTOHETEROCYCLIC COMPOUND CONTAINING A NITROGEN-CARBON DOUBLE BOND WITH WICH THE DISULFIDE LINKAGE IS CONJUGATED.

6. 发明申请

US20120277428A1 NEW COUPLING AGENTS FOR PEPTIDE SYNTHESIS 失效
标题翻译：用于肽合成的新型偶联剂
公开(公告)号：US20120277428A1
公开(公告)日：2012-11-01
申请号：US13544313
申请日：2012-07-09
申请人： Louis A. Carpino , Jusong Xia , Chongwu Zhang , Calin Dan Sferdean
发明人： Louis A. Carpino , Jusong Xia , Chongwu Zhang , Calin Dan Sferdean
IPC分类号： C07D487/04
CPC分类号： C07F9/6561 , C07D471/04 , C07F9/65188 , C07F9/65218 , C07F9/657163 , C07F9/65742 , C07K1/082 , C07K1/10
摘要： The present invention is directed to compounds of the formula: or salts thereof or N-oxides and their use in peptide synthesis.
摘要翻译：本发明涉及下式的化合物或其盐或N-氧化物及其在肽合成中的用途。

7. 再颁专利

USRE37686E1 Azahydroxybenzotriazoles and derivatives thereof for peptide coupling reactions 有权
标题翻译：氮杂羟基苯并三唑及其衍生物用于肽偶联反应
公开(公告)号：USRE37686E1
公开(公告)日：2002-04-30
申请号：US09213298
申请日：1998-12-03
申请人： Louis A. Carpino
发明人： Louis A. Carpino
IPC分类号： C07D48700
CPC分类号： C07D471/04 , C07D491/04 , C07D495/04 , C07D513/04 , C07F9/6561 , C07K1/082 , C07K1/084 , C07K1/10
摘要： This invention relates to a process for forming an amide or an ester from a reaction between an amine or an alcohol, respectively and an acylating derivative of a carboxylic acid, in the presence of an effective amount of a compound having the formula: and N-oxides thereof and salts thereof.
摘要翻译：本发明涉及一种在有效量的具有下式的化合物存在下，分别由胺或醇与羧酸的酰化衍生物反应形成酰胺或酯的方法：N- 氧化物及其盐。

8. 发明授权

US5644029A Reagents for peptide couplings 失效
公开(公告)号：US5644029A
公开(公告)日：1997-07-01
申请号：US468300
申请日：1995-06-06
申请人： Louis A. Carpino
发明人： Louis A. Carpino
IPC分类号： C07D471/04 , C07D491/04 , C07D491/048 , C07D495/04 , C07D498/04 , C07D513/04 , C07F9/6561 , C07K1/08 , C07K1/10 , C07K5/00
CPC分类号： C07F9/6561 , C07D471/04 , C07D491/04 , C07D495/04 , C07D513/04 , C07K1/082 , C07K1/084 , C07K1/10
摘要： This invention relates to a process for forming an amide or an ester from a reaction between an amine or an alcohol, respectively and an acylating derivative of a carboxylic acid, in the presence of an effective amount of a compound having the formula: ##STR1## and N-oxides thereof and salts thereof.

9. 发明授权

US3907855A Process for producing active esters of amino acids 失效
标题翻译：生产氨基酸活性酯的方法
公开(公告)号：US3907855A
公开(公告)日：1975-09-23
申请号：US42319673
申请日：1973-12-10
申请人： SUMITOMO CHEMICAL CO
发明人： YAMAZAKI NOBORU , HIGASHI FUKUJI
IPC分类号： C07C325/00 , C07C67/00 , C07C227/18 , C07C229/02 , C07C231/00 , C07C231/12 , C07C233/47 , C07C239/00 , C07C271/08 , C07C313/00 , C07C327/20 , C07K1/08 , C07C153/09
CPC分类号： C07K1/084 , C07K1/082
摘要： Active esters of amino acids having protected amino groups (hereinafter represented by ''''N-protected amino acids'''') are produced by reacting an N-protected amino acid with a compound having at least one hydroxyl or mercapto group in the presence of a phosphorous acid ester and a tertiary amine.
摘要翻译：具有被保护的氨基的氨基酸的活性酯（以下由“N-保护的氨基酸”表示）是通过N-保护的氨基酸与具有至少一个羟基或巯基的化合物在亚磷酸酯和叔胺。

10. 发明授权

US3120542A Imidazolephosphites 失效
标题翻译：亚硝酸咪唑
公开(公告)号：US3120542A
公开(公告)日：1964-02-04
申请号：US7115060
申请日：1960-11-23
申请人： AMERICAN CYANAMID CO
发明人： ANDERSON GEORGE W , YOUNG RICHARD W
IPC分类号： C07F9/6571 , C07K1/08
CPC分类号： C07F9/657154 , C07K1/082 , C07K1/084

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