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51. 发明公开

KR1020170023158A 2-아미노 치환 벤즈알데히드 화합물을 제조하는 방법 审中-实审
标题翻译： 2-生产2-氨基取代的苯甲醛化合物的方法
公开(公告)号：KR1020170023158A
公开(公告)日：2017-03-02
申请号：KR1020177002258
申请日：2015-08-25
申请人： 닛뽕소다 가부시키가이샤
发明人： 고바야시신이치
IPC分类号： C07C221/00 , C07C223/06
CPC分类号： C07C221/00 , C07B51/00 , C07B61/00 , C07C223/06 , C07D317/16 , C07D317/28
摘要： 본발명에의해, 할로게노기또는알콕시기가 3 위치에결합하고, 수소원자가 2 위치에결합하고, 또한리튬화반응이 2 위치에서가장활성이되도록, 수소원자, 알킬기, 할로게노기, 알콕시기혹은시아노기가 4 위치, 5 위치및 6 위치에각각독립적으로결합하고있는벤즈알데히드를준비하고, 그벤즈알데히드중의포르밀기를아세탈보호하고, 2 위치를순차리튬화, 아지화및 아미노화하고, 이어서, 아세탈탈보호하는것을포함하는, 아미노기가 2 위치에결합하고, 할로게노기또는알콕시기가 3 위치에결합하고또한수소원자, 알킬기, 할로게노기, 알콕시기혹은시아노기가 4 위치, 5 위치및 6 위치에각각독립적으로결합하고있는벤즈알데히드를제조하는방법이제공된다.
摘要翻译：本发明提供一种苯甲醛的制造方法，其中氨基在2位上键合，卤代基或烷氧基键合在3位，氢原子，烷基，卤代基，烷氧基或氰基分别独立地键合在4,5,6个位置，该方法包括：制备其中在3位上键合有卤代基或烷氧基的苯甲醛，氢原子键合在2位，氢原子，烷基，卤代基，烷氧基或氰基在4,5,6位中分别独立地键合，使得锂化反应在 2位; 在苯甲醛中缩醛保护甲酰基; 依次执行2位的锂化，叠氮化和胺化; 然后进行缩醛脱保护。

52. 发明申请

US20190185428A1 METHOD FOR PRODUCING CHIRAL AMINONITRILES 审中-公开
公开(公告)号：US20190185428A1
公开(公告)日：2019-06-20
申请号：US16328519
申请日：2017-08-17
申请人： UNIVERSITÄT BIELEFELD
发明人： Harald GRÖGER , Tobias BETKE , Philipp ROMMELMANN
IPC分类号： C07D207/16 , C07B51/00
CPC分类号： C07D207/16 , C07B51/00 , C07B2200/07
摘要： The invention relates to a method for preparing an N-acyl- or N-sulfonyl-α-aminonitrile, comprising the following steps: a) condensation of an N-acyl- or N-sulfonyl-α-aminoaldehyde with hydroxylamine to give an aldoxime, and b) dehydration of the aldoxime obtained in step a) to give an N-acyl- or N-sulfonyl-α-aminonitrile. In an advantageous manner, the absolute configuration can be retained in the conversion to the N-acyl- or N-sulfonyl-α-aminonitrile.

53. 发明申请

US20190185392A1 Carbon Dioxide as a Directing Group for C-H Functionalization Reactions Involving Lewis Basic Amines, Alcohols, Thiols, and Phosphines for the Synthesis of Compounds 审中-公开
公开(公告)号：US20190185392A1
公开(公告)日：2019-06-20
申请号：US16223467
申请日：2018-12-18
申请人： The University of Toledo
发明人： Michael C. Young , Mohit Kapoor
IPC分类号： C07B37/02 , C07B37/04 , C07B43/00 , C07C209/68 , C07C211/52 , C07C211/08 , B01J31/04 , C07B47/00
CPC分类号： C07B37/02 , B01J31/04 , B01J31/4038 , B01J2231/46 , B01J2531/824 , C07B37/04 , C07B43/00 , C07B47/00 , C07B51/00 , C07C209/68 , C07C211/08 , C07C211/52
摘要： Methods of synthesizing compounds using CO2 as a directing group for C—H functionalization, and compounds made thereby, are described.

54. 发明申请

US20180170949A1 SYNTHESIS OF CEPHALOSPORIN COMPOUNDS 审中-公开
公开(公告)号：US20180170949A1
公开(公告)日：2018-06-21
申请号：US15540283
申请日：2015-12-18
申请人： MERCK SHARP & DOHME CORP.
发明人： Kristos Adrian MOSHOS , Valdas JURKAUSKAS , Giovanni FOGLIATO , Manuel SCANU , Michele BENOTTI
IPC分类号： C07D501/56 , C07D417/14 , C07B43/04 , C07B43/06 , C07B51/00
CPC分类号： C07D501/56 , C07B43/04 , C07B43/06 , C07B51/00 , C07D417/14
摘要： Described herein are methods for the manufacture of ceftolozane and related compounds, as well as compositions comprising the same.

55. 发明授权

US09605020B2 Method for producing dipeptide derivative containing disubstituted amino acid residue 有权
公开(公告)号：US09605020B2
公开(公告)日：2017-03-28
申请号：US14914458
申请日：2014-08-20
申请人： NAGASE & CO., LTD.
发明人： Keisuke Matsuyama , Kazuya Kodama
IPC分类号： C07C229/00 , C07K5/065 , C07B51/00 , C07K5/062 , C07K5/072
CPC分类号： C07K5/06078 , C07B51/00 , C07K1/02 , C07K5/06026 , C07K5/06034 , C07K5/06043 , C07K5/0606 , C07K5/06095
摘要： A method for producing a dipeptide that has a protected N-terminal and is represented by formula (1) or a salt of the dipeptide, said method comprising condensing an α-monosubstituted amino acid that has a protected N-terminal and is represented by formula (2) or glycine or a salt thereof with a disubstituted amino acid that is represented by formula (3) or a salt thereof in the presence of a condensing agent [in each of the formulae, substituents are as defined in the description or the like].

56. 发明授权

US09604893B2 Protecting phenol groups 有权
公开(公告)号：US09604893B2
公开(公告)日：2017-03-28
申请号：US14895792
申请日：2014-05-12
申请人： Univation Technologies, LLC
发明人： C. Jeff Harlan , Steven D. Brown
IPC分类号： C08F2/00 , C08F4/60 , C07D315/00 , C07C41/00 , C07C41/18 , C07D309/30 , C07B51/00 , C07C41/01 , C07D309/12 , C08F210/02
CPC分类号： C07C41/18 , C07B51/00 , C07C41/01 , C07D309/12 , C07D309/30 , C08F210/02
摘要： A method for protecting a phenol group on a precursor compound is provided. The method includes reacting the phenol group with dihydropyran in an acid catalyzed protection reaction and quenching the protection reaction with a strong base within less than about 60 seconds to form a protected precursor compound.

57. 发明申请

US20140343281A1 HYDROXY GROUP PROTECTING AGENT AND HYDROXY GROUP PROTECTION METHOD 有权
标题翻译：羟基保护剂和羟基保护方法
公开(公告)号：US20140343281A1
公开(公告)日：2014-11-20
申请号：US14359183
申请日：2012-11-16
申请人： Munetaka Kunishima , Hikaru Fujita , Kohei Yamada
发明人： Munetaka Kunishima , Hikaru Fujita , Kohei Yamada
IPC分类号： C07D251/30 , C07C67/62
CPC分类号： C07D251/30 , C07B51/00 , C07C41/14 , C07C67/24 , C07C67/29 , C07C67/62 , C07C2601/14 , C07C2603/74 , C07D251/26 , C07D251/34 , Y02P20/55 , C07C43/164 , C07C69/616 , C07C69/157 , C07C43/188
摘要： To provide: a hydroxy group protecting agent which is stable and easy to use, does not have carcinogenicity, a tearing property or the like, and is inexpensive; and a hydroxy group protection method which enables the protection of a hydroxy group under acidic conditions.[Solution] A hydroxy group protecting agent in which at least one protecting group is bound to a nitrogen-containing electron-withdrawing heterocyclic ring through any one of an oxygen atom, a sulfur atom and a nitrogen atom. The heterocyclic ring is a triazine ring or the like, and the protecting group is a benzyl group or the like. Specifically, the hydroxy group protecting agent is 2,4,6-tribenzyloxy-1,3,5-triazine, 2,4,6-tris(4-methoxybenzyloxy)-1,3,5-triazine or the like. In addition, 2,4,6-tris(t-butoxy)-1,3,5-triazine or the like can also be used. For protecting a hydroxy group, a compound of interest which has a hydroxy group is reacted with the hydroxy group protecting agent under acidic conditions.
摘要翻译：提供：稳定且易于使用的羟基保护剂，不具有致癌性，撕裂性等，并且价格便宜; 以及能够在酸性条件下保护羟基的羟基保护方法。 [溶液]其中至少一个保护基通过氧原子，硫原子和氮原子中的任一个与含氮吸电子杂环结合的羟基保护剂。杂环是三嗪环等，保护基是苄基等。具体地，羟基保护剂是2,4,6-三苄氧基-1,3,5-三嗪，2,4,6-三（4-甲氧基苄氧基）-1,3,5-三嗪等。此外，也可以使用2,4,6-三（叔丁氧基）-1,3,5-三嗪等。为了保护羟基，具有羟基的目的化合物在酸性条件下与羟基保护剂反应。

58. 发明申请

US20110190475A1 PROCESSES FOR REMOVAL OF DIBENZOFULVENE 失效
标题翻译：去除二苯并呋喃的方法
公开(公告)号：US20110190475A1
公开(公告)日：2011-08-04
申请号：US13020838
申请日：2011-02-04
申请人： Yuji Nishiuchi , Terutoshi Kimura
发明人： Yuji Nishiuchi , Terutoshi Kimura
IPC分类号： C07K5/10
CPC分类号： C07B51/00 , C07B63/00 , C07C227/40 , C07C231/22 , C07K1/063 , C07K1/064 , C07K1/14 , C07C229/22 , C07C237/08
摘要： A dibenzofulvene amine adduct is removed by contacting a reaction mixture containing the dibenzofulvene amine adduct, which is obtained by reacting, for deprotection, an amino acid compound protected with an Fmoc group with an amine compound containing a nitrogen atom which is bonded to at least one hydrogen atom, with carbon dioxide, and removing the carbonate of the dibenzofulvene amine adduct. Alternatively, a dibenzofulvene amine adduct is removed by mixing a reaction mixture during a deprotection reaction of the amino acid compound protected with an Fmoc group, or after the reaction with an amine compound containing a nitrogen atom which is bonded to at least one hydrogen atom to give a mixture containing the dibenzofulvene amine adduct, contacting the mixture with carbon dioxide, and removing the carbonate of the dibenzofulvene amine adduct.
摘要翻译：通过使含有二苯并富烯胺加合物的反应混合物与通过与保护的Fmoc基保护的氨基酸化合物与含有氮原子的胺化合物反应获得的反应混合物除去二苯并富烯胺加合物，所述胺化合物与至少一个氢原子与二氧化碳反应，并除去二苯并富烯胺加合物的碳酸酯。或者，通过在用Fmoc基保护的氨基酸化合物的脱保护反应中或在与含有至少一个氢原子键合的氮原子的胺化合物反应后，将反应混合物混合，除去二苯并富烯胺加合物，得到含有二苯并富烯胺加合物的混合物，使混合物与二氧化碳接触，并除去二苯并富烯胺加合物的碳酸酯。

59. 发明授权

US07972836B2 Method of enzymatic optical resolution of racemic 4-hydroxy-1,2,3,4-tetrahydroquinoline 有权
标题翻译：外消旋4-羟基-1,2,3,4-四氢喹啉的酶学光学拆分方法
公开(公告)号：US07972836B2
公开(公告)日：2011-07-05
申请号：US12083014
申请日：2006-10-04
申请人： Masaki Okamoto , Akira Sakuragi , Muneki Kishida , Yoshikazu Mori
发明人： Masaki Okamoto , Akira Sakuragi , Muneki Kishida , Yoshikazu Mori
IPC分类号： C12P41/00 , C12P17/18
CPC分类号： C07D215/233 , C07B51/00 , C07B53/00 , C07D215/06 , C07D215/08 , C07D401/04 , C12P17/12 , C12P41/005 , Y02P20/55
摘要： The present invention relates to a method for preparing an optically active 4-hydroxy-1,2,3,4-tetrahydroquinoline compound [I], which comprises the steps of: treating a racemic 4-hydroxy-1,2,3,4-tetrahydroquinoline compound represented by general formula [I]: [wherein R1 represents a hydrogen atom or a protecting group for amino group.] with an enzyme having an ability of selectively or preferentially acylating one enantiomer of the racemic compound [I] in the presence of an acyl donor; and if necessary, subjecting the reaction product to solvolysis.
摘要翻译：本发明涉及一种制备光学活性4-羟基-1,2,3,4-四氢喹啉化合物[I]的方法，其包括以下步骤：将外消旋的4-羟基-1,2,3,4 通式[I]表示的四氢喹啉化合物：[其中R1表示氢原子或氨基保护基]与具有选择性或优先酰化外消旋化合物[I]的一种对映异构体的能力的酶在存在下的酰基供体; 并且如果需要，使反应产物溶解。

60. 发明申请

US20100233314A1 SOLVENT-FREE SYNTHESIS OF AMPHIPHILIC POLYMERIC MATERIAL 有权
标题翻译：无水聚合物的无溶剂合成
公开(公告)号：US20100233314A1
公开(公告)日：2010-09-16
申请号：US12733698
申请日：2008-10-15
申请人： Terence Cosgrove , Roger Pettman , Erol Hasan
发明人： Terence Cosgrove , Roger Pettman , Erol Hasan
IPC分类号： A23G4/08 , C08F222/06
CPC分类号： C08F8/10 , A23G4/08 , C07B51/00 , C08F8/32 , C08F236/02 , C08G63/91 , C08G81/025
摘要： The present invention provides a method for making a composition comprising an amphiphilic polymeric material which comprises a straight or branched chain carbon-carbon backbone and a multiplicity of side chains attached to the backbone; wherein in the method, backbone precursors comprising acylating groups are mixed with side chain precursors which comprise a nucleophilic group at at least one terminus, to form a reaction mixture; the backbone precursors, side chain precursors and/or the reaction mixture are heated; the reaction mixture is stirred; and the nucleophilic groups react with the acylating groups to form the amphilphilic polymeric material wherein the side chains are linked to the backbone via acyl linkages; characterised in that the reaction mixture does not comprise organic solvent.
摘要翻译：本发明提供一种制备包含两亲性聚合物材料的组合物的方法，所述两亲性聚合物材料包含直链或支链碳 - 碳骨架和连接至主链的多个侧链; 其中在该方法中，包含酰化基团的主链前体与至少在一个末端包含亲核基团的侧链前体混合以形成反应混合物; 骨架前体，侧链前体和/或反应混合物被加热; 搅拌反应混合物; 并且亲核基团与酰化基团反应以形成亲水性聚合物质，其中侧链通过酰基键连接至主链; 其特征在于反应混合物不包含有机溶剂。

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