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91. 发明公开

US20240059656A1 A TAUTOMERIC LIGAND ENABLES BIOMIMETIC C-H HYDROXYLATION WITH MOLECULAR OXYGEN 审中-公开
公开(公告)号：US20240059656A1
公开(公告)日：2024-02-22
申请号：US18256680
申请日：2021-12-09
申请人： THE SCRIPPS RESEARCH INSTITUTE
发明人： Jin-Quan YU , Zhen WANG , Zhen LI
IPC分类号： C07D213/803 , C07C51/373 , C07C227/10 , C07C231/12 , C07C303/40 , C07D209/08 , C07D209/26 , C07D209/86 , C07D213/55 , C07D213/61 , C07D213/643 , C07D213/69 , C07D213/74 , C07D215/48 , C07D215/50 , C07D235/20 , C07D241/42 , C07D271/06 , C07D277/64 , C07D295/155 , C07D307/79 , C07D307/91 , C07D319/18 , C07D333/54 , C07D333/76 , C07F15/00 , C07K5/065
CPC分类号： C07D213/803 , C07C51/373 , C07C227/10 , C07C231/12 , C07C303/40 , C07D209/08 , C07D209/26 , C07D209/86 , C07D213/55 , C07D213/61 , C07D213/643 , C07D213/69 , C07D213/74 , C07D215/48 , C07D215/50 , C07D235/20 , C07D241/42 , C07D271/06 , C07D277/64 , C07D295/155 , C07D307/79 , C07D307/91 , C07D319/18 , C07D333/54 , C07D333/76 , C07F15/0066 , C07K5/06078
摘要： Disclosed herein is a process for making a compound of formula (2) by (hetero)aromatic C—H hydroxylation of a compound of formula (1): catalyzed by palladium(II) and a bidentate ligand in the presence of O2. The process is useful for instance, in the late-stage modification of medicinally important heterocycles.

92. 发明授权

US10836717B2 Reagents for fluorosulfating alcohols or amines 有权
公开(公告)号：US10836717B2
公开(公告)日：2020-11-17
申请号：US16103824
申请日：2018-08-14
申请人： BIODURO, LLC , PFIZER, INC.
发明人： Hua Zhou , Paramita Mukherjee , Rongqiang Liu , Christopher W. Am Ende , Tianjing Deng
IPC分类号： C07C303/24 , C07C305/26 , C07C381/00 , C07B45/00 , C07D311/16 , C07D491/10 , C07D213/65 , C07D413/04 , C07C227/10 , C07C307/00 , C07D239/88 , C07D215/32 , C07D211/96 , C07D209/88 , C07D249/18
CPC分类号： C07C381/00 , C07B45/00 , C07C227/10 , C07C303/24 , C07C305/26 , C07C307/00 , C07D209/88 , C07D211/96 , C07D213/65 , C07D215/32 , C07D239/88 , C07D249/18 , C07D311/16 , C07D413/04 , C07D491/10 , C07C303/24 , C07C305/26 , C07C227/10 , C07C229/60
摘要： Disclosed herein are compounds of formula Ar—N(SO2F)2, wherein Ar is selected from an optionally substituted aryl, an optionally substituted five-membered heteroaryl, or an optionally substituted six-membered heteroaryl. Also disclosed are methods of synthesizing the above compounds by reacting a compound of formula Ar—NH—R9 with MN(SO2F)2.

93. 发明授权

US09376409B2 Methods for making oxetan-3-ylmethanamines 有权
标题翻译：制备氧杂环丁烷-3-基甲胺的方法
公开(公告)号：US09376409B2
公开(公告)日：2016-06-28
申请号：US14399343
申请日：2013-05-01
申请人： Boehringer Ingelheim International GmbH
发明人： Magnus Carl Arne Eriksson , Suresh R. Kapadia , Jonathan Timothy Reeves , Xingzhong Zeng
IPC分类号： C07D305/06 , C07C215/10 , C07C227/10 , C07C229/24 , C07C213/00 , C07C215/28 , C07C229/34
CPC分类号： C07D305/06 , C07C213/00 , C07C215/10 , C07C215/28 , C07C227/10 , C07C229/24 , C07C229/34
摘要： This invention relates to methods for making oxetan-3-ylmethanamines having the formula (I) wherein R1? and R2? are as defined herein. The methods of the invention provide the compounds of formula (I) in high yields and under conditions amenable for large-scale commercial production.
摘要翻译：本发明涉及制备具有式（I）的氧杂环丁烷-3-基甲胺的方法，和R2？如本文所定义。本发明的方法以高产率和适于大规模商业生产的条件提供式（I）化合物。

94. 发明申请

US20150353474A1 CARBOXYBETAINE-FUNCTIONALIZED DIOLS 有权
标题翻译：羧甲基功能二醇
公开(公告)号：US20150353474A1
公开(公告)日：2015-12-10
申请号：US14830911
申请日：2015-08-20
申请人： Peter N. Coneski , James H. Wynne
发明人： Peter N. Coneski , James H. Wynne
IPC分类号： C07C229/12 , C07C227/10
CPC分类号： C07C229/12 , C07C227/02 , C07C227/10 , C08G18/0833 , C08G18/3206 , C08G18/3804 , C08G18/381 , C08G18/3821 , C08G18/73 , C08G18/7831 , C08G18/791 , C08G18/792 , C08G18/82 , C08G2210/00 , Y02P20/55
摘要： A compound having the formula: X−N+(CH3)(CH2CH2OH)2[(CH2)n—COO—R1]. R1 is an ester protecting group, X is a halide, and n is a positive integer. A method of reacting N-methyldiethanolamine with an ω-halo-n-alkanoate ester to form the compound.
摘要翻译：具有下式的化合物：X-N +（CH3）（CH2CH2OH）2 [（CH2）n-COO-R1]。 R1是酯保护基，X是卤素，n是正整数。使N-甲基二乙醇胺与ω-卤代正丁酸酯反应形成化合物的方法。

95. 发明授权

US09090536B2 Process for the preparation of a mixture of chelating agents 有权
标题翻译：制备螯合剂混合物的方法
公开(公告)号：US09090536B2
公开(公告)日：2015-07-28
申请号：US13639575
申请日：2011-05-31
申请人： Reijo Aksela , Jussi Rissanen
发明人： Reijo Aksela , Jussi Rissanen
IPC分类号： C07C213/06 , C07C227/10 , C07C227/06 , C07C227/16
CPC分类号： C07C227/10 , C07C227/06 , C07C227/16 , C07C229/24
摘要： The present invention relates to a process for the preparation of a mixture of aspartic acid diethoxy succinate and an amino acid derivative of the general formula (I) wherein n is 1-10, m is 0 or 1, and R is hydrogen or an alkali metal or alkaline earth metal ion, comprising reacting maleate with diethanol amine under alkaline conditions in the presence of a lanthanoid catalyst to form aspartic acid diethoxy succinate followed by adding aspartic acid which reacts with unreacted maleate to form imino disuccinic acid, i.e. an amino acid derivative of formula (I) wherein m is 0, or by adding a diamine derivative of the general formula (II) NH2(CH2)nNH2 wherein n is as defined above, which reacts with unreacted maleate to form an amino acid derivative of formula (I) wherein m is 1 and n is as defined above.
摘要翻译：本发明涉及一种制备天冬氨酸二乙氧基琥珀酸酯与通式（I）的氨基酸衍生物的混合物的方法，其中n为1-10，m为0或1，R为氢或碱金属或碱土金属离子，包括在碱性条件下在镧系元素催化剂存在下使马来酸酯与二乙醇胺反应，形成天冬氨酸二乙氧基琥珀酸酯，然后加入与未反应的马来酸酯反应形成亚氨基二琥珀酸的天冬氨酸，即氨基酸衍生物或通过加入通式（II）的二胺衍生物NH 2（CH 2）n NH 2，其中n如上定义，其与未反应的马来酸酯反应以形成式（I）的氨基酸衍生物），其中m是1，n如上定义。

96. 发明申请

US20150112084A1 PROCESS FOR PREPARATION OF (IS, 3S, 5S)-2-[(2S)-2-AMIN0-2-(3-HYDROXY-l-ADAMANTYL) ACETYL]-2-AZABICYCLO [3.1.0] HEXANE-3-CARBONITRILE 有权
标题翻译：（1S，3S，5S）-2 - [（2S）-2-氨基-2-（3-羟基-1-亚氨基）乙酰基] -2-亚甲基] [3.1.0]异丙基-3-碳二烯的制备方法
公开(公告)号：US20150112084A1
公开(公告)日：2015-04-23
申请号：US14404686
申请日：2013-04-22
申请人： RAMAMOHAN RAO DAVULURI
发明人： Ponniah Ravi , Praveen Kumar Neela , Batthini Guruswamy , Sribashyam Ravikanth , Uppala Manikya Rao , Dongari Naresh , Mogili Ravindar
IPC分类号： C07D209/52 , C07C229/28 , C07C227/16 , C07C247/12 , C07C227/10
CPC分类号： C07D209/52 , C07C227/10 , C07C227/16 , C07C229/28 , C07C247/12
摘要： Provided are novel processes for the preparation of Saxagliptin and novel intermediates employed in the process for preparing Saxagliptin.
摘要翻译：提供了用于制备沙格列汀的新方法和用于制备萨格列汀的方法中使用的新型中间体。

97. 发明授权

US08952190B2 Synergists 有权
标题翻译：协同主义者
公开(公告)号：US08952190B2
公开(公告)日：2015-02-10
申请号：US13636971
申请日：2011-03-25
申请人： Robert Stephen Davidson , Shaun Lawrence Herlihy
发明人： Robert Stephen Davidson , Shaun Lawrence Herlihy
IPC分类号： C07C229/00 , C07C229/18 , C07C227/10 , C08F2/48 , C09D11/101
CPC分类号： C07C229/18 , C07C227/10 , C07C2602/42 , C07C2603/68 , C08F2/48 , C09D11/101
摘要： Compounds of formula (I): wherein Ar represents an, optionally substituted, aryl or heteroaryl group, R represents an, optionally substituted, aryl or heteroaryl group, an optionally substituted straight or branched chain C1.10-alkyl, R1 is H or methyl, X is an extender group, n is 0 or an integer between 1 and 12 inclusive, A is a polyol residue wherein the unsubstituted polyol from which the residue is derived has at least y OH groups, and y is an integer>1, can easily be prepared, and are useful as synergists in radiation curing.
摘要翻译：式（I）化合物：其中Ar表示任选取代的芳基或杂芳基，R表示任选取代的芳基或杂芳基，任选取代的直链或支链C 1-10 - 烷基，R 1为H或甲基 X为增量基团，n为0或1〜12的整数，A为多元醇残基，其中，残基得到的未取代的多元醇至少具有y OH基，y为1以上的整数，易于制备，并且可用作辐射固化中的增效剂。

98. 发明申请

US20140135519A1 CARBOXYLIC ACID ESTER PRODRUG INHIBITORS OF MEK 有权
标题翻译：羧甲基酯酸酯抑制剂
公开(公告)号：US20140135519A1
公开(公告)日：2014-05-15
申请号：US14081426
申请日：2013-11-15
申请人： DUQUESNE UNIVERSITY OF THE HOLY GHOST
发明人： SURAVI CHAKRABARTY , Darlene Monlish , Patrick Flaherty , Jane E. Cavanaugh , Sneha Potdar
IPC分类号： C07C229/64 , C07C227/10
CPC分类号： C07C227/10 , C07C229/58
摘要： The invention generally relates to compounds having structure I: wherein x represents alkyl, aryl or het-aryl, each of y independently represents hydrogen or halogen and z represents hydrogen or alkyl. Further, said compounds are inhibitors of MEK 1, 2 and 5. Furthermore, the invention includes methods of making said compounds, compositions including said compounds and uses for inhibiting MEK 1, 2 and 5.
摘要翻译：本发明一般涉及具有结构I的化合物：其中x代表烷基，芳基或苯基 - 芳基，y各自独立地表示氢或卤素，z代表氢或烷基。此外，所述化合物是MEK 1,2和5的抑制剂。此外，本发明包括制备所述化合物，包含所述化合物的组合物和用于抑制MEK 1,2和5的方法。

99. 发明申请

US20140024768A1 CARBOXYBETAINE-FUNCTIONALIZED DIOLS AND ZWITTERIONIC POLYURETHANE HYDROGELS DERIVED THEREFROM 有权
标题翻译：羧甲基官能化二醇和其衍生的聚氨酯水凝胶
公开(公告)号：US20140024768A1
公开(公告)日：2014-01-23
申请号：US13783481
申请日：2013-03-04
申请人： Peter N. Coneski , James H. Wynne
发明人： Peter N. Coneski , James H. Wynne
IPC分类号： C08G18/38 , C07C227/10 , C07C229/12
CPC分类号： C07C229/12 , C07C227/02 , C07C227/10 , C08G18/0833 , C08G18/3206 , C08G18/3804 , C08G18/381 , C08G18/3821 , C08G18/73 , C08G18/7831 , C08G18/791 , C08G18/792 , C08G18/82 , C08G2210/00 , Y02P20/55
摘要： A compound having the formula: X−N+(CH3)(CH2CH2OH)2[(CH2)n—COO—R1] and a polymer having the repeat unit: X−{—OCH2CH2—N+(CH3)[(CH2)n—CO—Y]—CH2CH2O—CO—NH—R2—NH—CO—}. R1 is an ester protecting group, R2 is an organic group, X is a halide, and n is a positive integer. Each Y is O−Z+ or O—R1, where Z+ is a cation from an aqueous base. A method of reacting N-methyldiethanolamine with an ω-halo-n-alkanoate ester to form the above compound.
摘要翻译：具有下式的化合物：X-N +（CH3）（CH2CH2OH）2 [（CH2）n-COO-R1]和具有重复单元的聚合物：X - { - OCH2CH2-N +（CH3）[（CH2）n- CO-Y] -CH2CH2O-CO-NH-R2-NH-CO-}。 R1是酯保护基，R2是有机基团，X是卤化物，n是正整数。每个Y是O-Z +或O-R1，其中Z +是碱性水溶液的阳离子。使N-甲基二乙醇胺与ω-卤代正丁酸酯反应形成上述化合物的方法。

100. 发明申请

US20130204035A1 PROCESS FOR THE PREPARATION OF A MIXTURE OF CHELATING AGENTS 有权
标题翻译：制备混合剂混合物的方法
公开(公告)号：US20130204035A1
公开(公告)日：2013-08-08
申请号：US13639575
申请日：2011-05-30
申请人： Reijo Aksela , Jussi Rissanen
发明人： Reijo Aksela , Jussi Rissanen
IPC分类号： C07C227/10
CPC分类号： C07C227/10 , C07C227/06 , C07C227/16 , C07C229/24
摘要： The present invention relates to a process for the preparation of a mixture of aspartic acid diethoxy succinate and an amino acid derivative of the general formula (I) wherein n is 1-10, m is 0 or 1, and R is hydrogen or an alkali metal or alkaline earth metal ion, comprising reacting maleate with diethanol amine under alkaline conditions in the presence of a lanthanoid catalyst to form aspartic acid diethoxy succinate followed by adding aspartic acid which reacts with unreacted maleate to form imino disuccinic acid, i.e. an amino acid derivative of formula (I) wherein m is 0, or by adding a diamine derivative of the general formula (II) NH2(CH2)nNH2 wherein n is as defined above, which reacts with unreacted maleate to form an amino acid derivative of formula (I) wherein m is 1 and n is as defined above.
摘要翻译：本发明涉及一种制备天冬氨酸二乙氧基琥珀酸酯与通式（I）的氨基酸衍生物的混合物的方法，其中n为1-10，m为0或1，R为氢或碱金属或碱土金属离子，包括在碱性条件下在镧系元素催化剂存在下使马来酸酯与二乙醇胺反应，形成天冬氨酸二乙氧基琥珀酸酯，然后加入与未反应的马来酸酯反应形成亚氨基二琥珀酸的天冬氨酸，即氨基酸衍生物或通过加入通式（II）的二胺衍生物NH 2（CH 2）n NH 2，其中n如上定义，其与未反应的马来酸酯反应以形成式（I）的氨基酸衍生物），其中m是1，n如上定义。

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