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1. 发明授权

US09126954B2 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：US09126954B2
公开(公告)日：2015-09-08
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： C07D251/34 , C07D251/30 , C07C41/14 , C07B51/00 , C07C67/24 , C07C67/29 , C07C67/62 , C07D251/26
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。

2. 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。

3. 发明申请

US20090023003A1 Molecular Aggregate Capable of Undergoing Phase Transition by Dehydrating Condensation and Method of Phase Transition Thereof 有权
标题翻译：通过脱水缩合进行相变的分子聚集体及其相转移方法
公开(公告)号：US20090023003A1
公开(公告)日：2009-01-22
申请号：US11814901
申请日：2005-12-12
申请人： Munetaka Kunishima
发明人： Munetaka Kunishima
IPC分类号： B01J13/02
CPC分类号： A61K9/1277 , A61K9/127 , B01J13/02 , B01J13/12 , Y10T428/1352 , Y10T428/2984 , Y10T428/31761
摘要： Provided is a bilayer membrane vesicle capable of undergoing a phase transition. The bilayer membrane vesicle includes: (a) a fatty acid salt having 6 to 20 carbon atoms; (b) an alcohol or an amine compound having an aliphatic chain of 6 to 20 carbon atoms; and (c) an artificial synthetic lipid or a phospholipid capable of forming a bilayer membrane. Preferably, this bilayer membrane vesicle further contains (d) a tertiary amine as a component of the membrane. Also provided is a method of inducing a phase transition of a bilayer membrane vesicle, the method including the step of adding a dehydrating condensing agent or a dehydrating condensing agent precursor having the property of accumulating at an interface to the bilayer membrane vesicle. By causing the lipids that form a molecular aggregate to chemically change, it is possible to change the physical property and the morphology of the molecular aggregate and control the timing of phase transitions such as membrane fusion. In the membrane fusion, for example, fusion can occur without leakage of the contents of the bilayer membrane vesicle.
摘要翻译：提供能够进行相变的双层膜囊泡。双层膜泡囊包括：（a）具有6至20个碳原子的脂肪酸盐; （b）具有6至20个碳原子的脂族链的醇或胺化合物; 和（c）能够形成双层膜的人造合成脂质或磷脂。优选地，该双层膜泡囊还含有（d）作为膜的组分的叔胺。还提供了诱导双层膜囊泡相变的方法，该方法包括以下步骤：将具有在界面处积累的性质的脱水缩合剂或脱水缩合剂前体添加到双层膜泡囊。通过使形成分子聚集体的脂质发生化学变化，可以改变分子聚集体的物理性质和形态，并且控制相变如时间的融合。例如，在膜融合中，可以发生融合，而不会泄漏双层膜囊泡的内容物。

4. 发明授权

US08449979B2 Molecular aggregate capable of undergoing phase transition by dehydrating condensation and method of phase transition thereof 有权
标题翻译：能够通过脱水缩合进行相变的分子聚集体及其相变化方法
公开(公告)号：US08449979B2
公开(公告)日：2013-05-28
申请号：US11814901
申请日：2005-12-12
申请人： Munetaka Kunishima
发明人： Munetaka Kunishima
IPC分类号： A61K38/08 , C07K7/00
CPC分类号： A61K9/1277 , A61K9/127 , B01J13/02 , B01J13/12 , Y10T428/1352 , Y10T428/2984 , Y10T428/31761
摘要： Provided is a bilayer membrane vesicle capable of undergoing a phase transition. The bilayer membrane vesicle includes: (a) a fatty acid salt having 6 to 20 carbon atoms; (b) an alcohol or an amine compound having an aliphatic chain of 6 to 20 carbon atoms; and (c) an artificial synthetic lipid or a phospholipid capable of forming a bilayer membrane. Preferably, this bilayer membrane vesicle further contains (d) a tertiary amine as a component of the membrane. Also provided is a method of inducing a phase transition of a bilayer membrane vesicle, the method including the step of adding a dehydrating condensing agent or a dehydrating condensing agent precursor having the property of accumulating at an interface to the bilayer membrane vesicle. By causing the lipids that form a molecular aggregate to chemically change, it is possible to change the physical property and the morphology of the molecular aggregate and control the timing of phase transitions such as membrane fusion. In the membrane fusion, for example, fusion can occur without leakage of the contents of the bilayer membrane vesicle.
摘要翻译：提供能够进行相变的双层膜囊泡。双层膜泡囊包括：（a）具有6至20个碳原子的脂肪酸盐; （b）具有6至20个碳原子的脂族链的醇或胺化合物; 和（c）能够形成双层膜的人造合成脂质或磷脂。优选地，该双层膜泡囊还含有（d）作为膜的组分的叔胺。还提供了诱导双层膜囊泡相变的方法，该方法包括以下步骤：将具有在界面处积累的性质的脱水缩合剂或脱水缩合剂前体添加到双层膜泡囊。通过使形成分子聚集体的脂质发生化学变化，可以改变分子聚集体的物理性质和形态，并且控制相变如时间的融合。例如，在膜融合中，可以发生融合，而不会泄漏双层膜囊泡的内容物。

5. 发明申请

US20070135632A1 Dehydrating condensation agent having property of accumulating at interface with water 有权
标题翻译：脱水缩合剂，其具有在与水的界面积聚的性质
公开(公告)号：US20070135632A1
公开(公告)日：2007-06-14
申请号：US10588940
申请日：2005-01-31
申请人： Munetaka Kunishima
发明人： Munetaka Kunishima
IPC分类号： C07D251/40
CPC分类号： C07D251/46 , C07C67/08 , C07C231/02 , C07C69/24
摘要： The present invention provides a 1,3,5-triazine compound represented by the following formula I: This compound can be synthesized easily and more economically and can be used as a dehydrating condensing agent having the property of accumulating at a water interface; In the case where carboxylic acid, amine, alcohol or other reaction substrate is amphiphilic, when mixing the dehydrating condensing agent of the present invention, which is amphiphilic, and the substrate to form various molecular aggregate phase including micelles in an aqueous solution, the substrate and the dehydrating condensing agent can be accumulated at the water interface. As a result, the concentration of the substrate increases locally at the water interface, and condensation reaction can be performed extremely efficiently.
摘要翻译：本发明提供由下式I表示的1,3,5-三嗪化合物：该化合物可以容易且更经济地合成，可用作具有在水界面积聚的性质的脱水缩合剂; 在羧酸，胺，醇或其它反应底物是两亲性的情况下，当混合本发明的两亲性脱水缩合剂和底物以在水溶液中形成包含胶束的各种分子聚集相时，脱水缩合剂可以在水界面积聚。结果，在水界面处，基板的浓度局部增加，并且可以非常有效地进行缩合反应。

6. 发明授权

US07462715B2 Dehydrating condensation agent having property of accumulating at interface with water 有权
标题翻译：脱水缩合剂，其具有在与水的界面积聚的性质
公开(公告)号：US07462715B2
公开(公告)日：2008-12-09
申请号：US10588940
申请日：2005-01-31
申请人： Munetaka Kunishima
发明人： Munetaka Kunishima
IPC分类号： C07D251/46 , C07C67/08 , C07C69/24 , C07C231/02 , C07C233/05
CPC分类号： C07D251/46 , C07C67/08 , C07C231/02 , C07C69/24
摘要： The present invention provides a 1,3,5-triazine compound represented by the following formula I: This compound can be synthesized easily and more economically and can be used as a dehydrating condensing agent having the property of accumulating at a water interface. In the case where carboxylic acid, amine, alcohol or other reaction substrate is amphiphilic, when mixing the dehydrating condensing agent of the present invention, which is amphiphilic, and the substrate to form various molecular aggregate phase including micelles in an aqueous solution, the substrate and the dehydrating condensing agent can be accumulated at the water interface. As a result, the concentration of the substrate increases locally at the water interface, and condensation reaction can be performed extremely efficiently.
摘要翻译：本发明提供由下式I表示的1,3,5-三嗪化合物：该化合物可以容易且更经济地合成，可用作具有在水界面积聚的性质的脱水缩合剂。在羧酸，胺，醇或其它反应底物是两亲性的情况下，当混合本发明的两亲性脱水缩合剂和底物以在水溶液中形成包含胶束的各种分子聚集相时，脱水缩合剂可以在水界面积聚。结果，在水界面处，基板的浓度局部增加，并且可以非常有效地进行缩合反应。

7. 发明授权

US06458948B1 Process for producing carboxylic acid derivative and condensing agent comprising quaternary ammonium salt 有权
标题翻译：制备含季铵盐的羧酸衍生物和缩合剂的方法
公开(公告)号：US06458948B1
公开(公告)日：2002-10-01
申请号：US09674930
申请日：2000-12-11
申请人： Fumiaki Iwasaki , Shohei Tani , Munetaka Kunishima , Keiji Terao , Michiko Miharu , Naoki Hirano , Masako Saijyo
发明人： Fumiaki Iwasaki , Shohei Tani , Munetaka Kunishima , Keiji Terao , Michiko Miharu , Naoki Hirano , Masako Saijyo
IPC分类号： C07D25146
CPC分类号： C07D401/04 , C07C67/08 , C07C231/02 , C07C319/20 , C07D207/16 , C07D251/46 , C07D453/02 , C07D501/00 , C07K1/10 , C07K5/06017 , C07K5/06026 , C07K5/06043 , C07K5/06078 , C07C323/59 , C07C233/11
摘要： A method of preparing carboxylic acid derivatives comprising mixing a quaternary ammonium salt having a particular triazine ring in the molecules thereof, a carboxylic acid compound and a compound having a nucleophilic functional group, to condense the carboxylic acid with the compound having the nucleophilic functional group. The invention further provides a condensing agent comprising the quaternary ammonium salt. The condensation is conducted under mild conditions to form carboxylic acid derivatives and, particularly, amide compounds or ester compounds maintaining high yields.
摘要翻译：一种制备羧酸衍生物的方法，包括在其分子中混合具有特定三嗪环的季铵盐，羧酸化合物和具有亲核官能团的化合物，以将羧酸与具有亲核官能团的化合物缩合。本发明还提供了包含季铵盐的缩合剂。缩合在温和条件下进行以形成羧酸衍生物，特别是保持高产率的酰胺化合物或酯化合物。

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