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公开(公告)号：KR1020090015231A
公开(公告)日：2009-02-12
申请号：KR1020070079373
申请日：2007-08-08
Applicant: 재단법인서울대학교산학협력재단
IPC: C07D243/14
Abstract: A manufacturing method of novel tetrahydro-1,4-benzodiazepin-5-one derivative and solid-phase thereof is provided to improve the purity and yield of compound through the single step conversion, thereby simultaneously manufacturing various kinds of compound libraries. The manufacturing method of tetrahydro-1,4-benzodiazepin-5-one derivative represented by the formula(1) comprises the steps of: reacting bromoacetal resin with primary amine to prepare secondary amine; coupling the secondary amine with anthranilic acid in which R3 is substituted; reacting the reaction product with aldehyde or ketone; and reacting the reaction product with formic acid to induce intramolecular cyclization.
Abstract translation: 提供新的四氢-1,4-苯并二氮杂-5-酮衍生物及其固相的制备方法，以通过单步转化提高化合物的纯度和产率，从而同时制备各种化合物文库。 由式（1）表示的四氢-1,4-苯并二氮杂-5-酮衍生物的制备方法包括以下步骤：使溴缩醛树脂与伯胺反应制备仲胺; 将仲胺与其中R3被取代的邻氨基苯甲酸偶联; 使反应产物与醛或酮反应; 并使反应产物与甲酸反应以诱导分子内环化。
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公开(公告)号：KR100876111B1
公开(公告)日：2008-12-26
申请号：KR1020070056687
申请日：2007-06-11
Applicant: 재단법인서울대학교산학협력재단
IPC: D06M11/42 , D06M13/144 , B82Y40/00 , D06M11/83
Abstract: A manufacturing method of antibacterial fiber in which nanosilver particle is coated is provided to control arbitrarily a size and a thickness of nanosilver particle coated on the fiber by controlling a relative concentration of a reactant. A manufacturing method of antibacterial fiber in which nanosilver particle is coated comprises a step of coating the nanosilver particle on fiber containing an alcohol functional group using a mixture including silver ion and aliphatic group or an aromatic amine compound. A pKa of the aliphatic group or the aromatic amine compound is 5 or greater. A relative concentration of the aliphatic amine compound and the silver ion is 1:0.1 or 1:5. A total concentration of the aliphatic amine compound and the silver ion is 10^-6 - 1 mol/liter.
Abstract translation: 提供其中涂覆有纳米银粒子的抗菌纤维的制造方法，以通过控制反应物的相对浓度来任意地控制涂覆在纤维上的纳米银粒子的尺寸和厚度。 其中涂覆有纳米银颗粒的抗菌纤维的制造方法包括使用包含银离子和脂族基团的混合物或芳族胺化合物将纳米银颗粒涂覆在含有醇官能团的纤维上的步骤。 脂肪族基团或芳香族胺化合物的pKa为5以上。 脂族胺化合物和银离子的相对浓度为1:0.1或1:5。 脂族胺化合物和银离子的总浓度为10 ^ -6-1mol / l。
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公开(公告)号：KR1020090070066A
公开(公告)日：2009-07-01
申请号：KR1020070137942
申请日：2007-12-26
Applicant: 재단법인서울대학교산학협력재단
IPC: C07D241/08 , C07D413/10
Abstract: A synthesis method of Delta5-2-oxopiperazine derivatives by the cyclization of N-acyliminium-ion is provided to apply to a building block and synthesize the Delta5-2-oxopiperazine library member with high yield and purity. A solid phase synthesis method of Delta5-2-oxopiperazine derivatives of the chemical formula 1 comprises: a step of reacting bromoacetal resin with a first amine compound to obtain a second amine compound; a step of coupling the second amine compound with R2-substituted amino acid to obtain a compound (7); a step of removing a protection group by reacting the compound (7) with piperidine to obtain a compound (8); and a step of reacting the compound with formic acid to obtain a compound (9). The R3 compound has a R3 substitution group of acetyl, carbonyl, carbamate, nitro benzoate or amino group.
Abstract translation: 提供了通过N-酰亚胺鎓离子的环化形成的Delta5-2-氧代哌嗪衍生物的合成方法，以适用于构建单元并以高产率和纯度合成Delta5-2-氧代哌嗪文献成员。 化学式1的δ5-2-氧代哌嗪衍生物的固相合成方法包括：使溴缩醛树脂与第一胺化合物反应得到第二胺化合物的步骤; 将第二胺化合物与R2取代的氨基酸偶联以获得化合物（7）的步骤; 通过使化合物（7）与哌啶反应以除去保护基团以获得化合物（8）的步骤; 和使化合物与甲酸反应得到化合物（9）的步骤。 R3化合物具有乙酰基，羰基，氨基甲酸酯，硝基苯甲酸酯或氨基的R3取代基。
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公开(公告)号：KR100799246B1
公开(公告)日：2008-01-29
申请号：KR1020060127039
申请日：2006-12-13
Applicant: 재단법인서울대학교산학협력재단
IPC: C07D491/048 , C07D491/147
CPC classification number: C07D491/052 , C07D311/04 , C07D491/107 , C07D491/147 , C07D491/20
Abstract: Compounds with an embedded benzopyran motif as core structures are provided to inhibit growth of cancer cells, so that they are useful for treatment of cancer. A preparation method of the compounds is also provided to improve convenience of preparation by using aqueous phase synthesis and solid phase synthesis. Compounds with an embedded benzopyran motif as core structures, represented by the formula(1) to formula(10) are provided, wherein Y and Z are each independently hydrogen; C1-C6 linear or branched alkyl; hydroxy; protected hydroxy as a C3-C9 linear or branched alkylsilyl ether type; halogen; C1-C6 linear or branched alkoxy; or phenyl optionally substituted by at least one selected from C1-C6 linear or branched alkyl, C1-C6 linear or branched alkoxy, hydroxy, hydroxy protected as a C3-C9 linear or branched alkylsilyl ether type, halogen, amino, C1-C4 alkylamino, C1-C4 dialkylamino, acetyl or benzoyl; R1 is hydrogen; methoxymethyl; C1-C6 linear or branched alkyl; benzyl; C1-C6 linear or branched alkoxy; or phenyl optionally substituted by at least one selected from C1-C6 linear or branched alkyl, C1-C6 linear or branched alkoxy, hydroxy, halogen, amino, C1-C4 alkylamino, C1-C4 dialkylamino, acetyl or benzoyl; and R is methyl or -CH2(CH2)2CH2-.
Abstract translation: 提供具有嵌入的苯并吡喃基序作为核心结构的化合物以抑制癌细胞的生长，使得它们可用于治疗癌症。 还提供了该化合物的制备方法，以通过使用水相合成和固相合成来提高制备的便利性。 提供了由式（1）至式（10）表示的具有嵌入的苯并吡喃基序作为核心结构的化合物，其中Y和Z各自独立地为氢; C1-C6直链或支链烷基; 羟基; 保护的羟基为C 3 -C 9直链或支链烷基甲硅烷基醚型; 卤素; C1-C6直链或支链烷氧基; 或任选被至少一个选自C 1 -C 6直链或支链烷基，C 1 -C 6直链或支链烷氧基，羟基，C 3 -C 9直链或支链烷基甲硅烷基醚保护的羟基取代的苯基，卤素，氨基，C 1 -C 4烷基氨基 ，C 1 -C 4二烷基氨基，乙酰基或苯甲酰基; R1是氢; 甲氧基甲基; C1-C6直链或支链烷基; 苄基; C1-C6直链或支链烷氧基; 或任选被至少一个选自C 1 -C 6直链或支链烷基，C 1 -C 6直链或支链烷氧基，羟基，卤素，氨基，C 1 -C 4烷基氨基，C 1 -C 4二烷基氨基，乙酰基或苯甲酰基取代的苯基; 且R为甲基或-CH 2（CH 2）2 CH 2 - 。
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公开(公告)号：KR100954561B1
公开(公告)日：2010-04-22
申请号：KR1020080039873
申请日：2008-04-29
Applicant: 재단법인서울대학교산학협력재단
IPC: C09K11/06
Abstract: 본 발명은 신규한 방사성 형광 화합물, 그 제조방법 및 그의 이용에 관한 것으로, 보다 상세하게는 1,2-디하이드로피롤로[3,4-β]인돌리진-3-온이라는 새로운 코어 스켈레톤(core skeleton)을 이용한 풀 컬러 조정가능한 방사성 형광 화합물, 그 제조방법 및 그 이용에 관한 것이다.
형광 화합물, 1,2-디히드로피롤로[3,4-β]인돌리진-3-온, 형광체, 바이오 프로브-
Patent Agency Ranking
公开(公告)号：KR100901316B1
公开(公告)日：2009-06-09
申请号：KR1020070079373
申请日：2007-08-08
Applicant: 재단법인서울대학교산학협력재단
IPC: C07D243/14
Abstract: 본 발명은 신규한 테트라하이드로-1,4-벤조디아제핀-5-온 유도체 및 고체상 평형 합성법을 이용하여 상기한 화합물을 고효율로 합성하는 방법에 관한 것이다.
테트라하이드로-1,4-벤조디아제핀-5-온, 고체상 합성, Leuckart-Wallach 반응, 브로모아세탈 수지-
公开(公告)号：KR1020080108736A
公开(公告)日：2008-12-16
申请号：KR1020070056687
申请日：2007-06-11
Applicant: 재단법인서울대학교산학협력재단
IPC: D06M11/42 , D06M13/144 , B82Y40/00 , D06M11/83
CPC classification number: D06M11/42 , B82Y40/00 , D06M11/83 , D06M13/144 , D10B2401/13 , D10B2509/022 , D10B2509/024
Abstract: A manufacturing method of antibacterial fiber in which nanosilver particle is coated is provided to control arbitrarily a size and a thickness of nanosilver particle coated on the fiber by controlling a relative concentration of a reactant. A manufacturing method of antibacterial fiber in which nanosilver particle is coated comprises a step of coating the nanosilver particle on fiber containing an alcohol functional group using a mixture including silver ion and aliphatic group or an aromatic amine compound. A pKa of the aliphatic group or the aromatic amine compound is 5 or greater. A relative concentration of the aliphatic amine compound and the silver ion is 1:0.1 or 1:5. A total concentration of the aliphatic amine compound and the silver ion is 10^-6 - 1 mol/liter.
Abstract translation: 提供其中涂覆有纳米银颗粒的抗菌纤维的制造方法，通过控制反应物的相对浓度来任意地控制涂覆在纤维上的纳米银颗粒的尺寸和厚度。 包含纳米银颗粒的抗菌纤维的制造方法包括使用包含银离子和脂肪族基团或芳香族胺化合物的混合物将纳米银粒子涂布在含有醇官能团的纤维上的工序。 脂肪族基团或芳香族胺化合物的pKa为5以上。 脂族胺化合物和银离子的相对浓度为1:0.1或1:5。 脂族胺化合物和银离子的总浓度为10 -6 -6 mol / L。
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公开(公告)号：KR1020080087301A
公开(公告)日：2008-10-01
申请号：KR1020070029334
申请日：2007-03-26
Applicant: 재단법인서울대학교산학협력재단
IPC: C07H3/00
CPC classification number: C07H3/00
Abstract: A glucose derivative is provided to show excellent capability as a glucose absorption tracer compared to a conventional 2-NBDG and monitor the glucose absorption in a normal culture medium state, thereby being usefully used for molecular imaging, bio-analysis, and screening a drug for treating or preventing glucose metabolism related diseases. A glucose derivative labeled with a fluorescent dye is represented by a formula(1) or (2), wherein R1 is -(CH2)n-NH- or -(CH2)n-NH-(C2H4X)m-NH-(wherein n is an integer from 1 to 10, m is an integer from 1 to 100, and X may be same or different from one another when the m is at least 2 and X is CH2, O or a single bond); R2 is a fluorescent dye; and Y is O or S. A method for synthesizing the glucose derivative of the formula(1) or (2) is characterized in that the fluorescent dye is labeled through O-1-glycosylation. A method for molecular imaging is characterized in that the glucose derivative labeled with the fluorescent dye is used as a bio-probe. A method for high throughput screening of a drug for treating or preventing glucose metabolism related diseases is characterized in that the glucose derivative labeled with the fluorescent dye is used as a probe.
Abstract translation: 提供葡萄糖衍生物以与常规的2-NBDG相比作为葡萄糖吸收示踪剂具有优异的能力，并监测正常培养基状态下的葡萄糖吸收，从而有效地用于分子成像，生物分析和筛选药物 治疗或预防葡萄糖代谢相关疾病。 用荧光染料标记的葡萄糖衍生物由式（1）或（2）表示，其中R1是 - （CH2）n-NH-或 - （CH2）n-NH-（C2H4X）m-NH-（其中 n为1〜10的整数，m为1〜100的整数，当m为2以上且X为CH 2，O或单键时，X可以相同或不同。 R2是荧光染料; 并且Y是O或S.用于合成式（1）或（2）的葡萄糖衍生物的方法的特征在于荧光染料通过O-1-糖基化被标记。 用于分子成像的方法的特征在于，用荧光染料标记的葡萄糖衍生物用作生物探针。 用于治疗或预防葡萄糖代谢相关疾病的药物的高通量筛选的方法的特征在于，用荧光染料标记的葡萄糖衍生物用作探针。
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公开(公告)号：KR100712667B1
公开(公告)日：2007-05-02
申请号：KR1020060032908
申请日：2006-04-11
Applicant: 재단법인서울대학교산학협력재단
IPC: C07D487/18 , C07D487/08
Abstract: 본 발명은 신규한 디아자 헤테로고리 유도체 및 그의 고체상 제조방법에 관한 것으로, 상세하게는 브로모아세탈 수지 고체상을 출발물질로 하여 아미노산과 다양한 유도체를 반응시킨 후 산성 조건에서 픽텟-스펭글러(Pictet-Spengler) 메커니즘을 이용하여 일용기반응(one-pot reaction)에서 고체상에서의 탈착과 목적 화합물을 얻는 것을 특징으로 한다.
Abstract translation: 本发明涉及新的杂环衍生物和二氮杂涉及其固相法，并且更尤其是溴用各种氨基酸衍生物的固相如在酸性条件格勒起始原料piktet缩醛树脂反应（Pictet- 斯宾格勒机理在一锅反应中在固相中获得解吸并获得目标化合物。
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公开(公告)号：KR100967171B1
公开(公告)日：2010-07-05
申请号：KR1020070137942
申请日：2007-12-26
Applicant: 재단법인서울대학교산학협력재단
IPC: C07D241/08 , C07D413/10
Abstract: 본 발명은 Δ
5 -2-옥소피페라진 유도체 및
N -아실이미늄 이온 고리화에 의해 상기 Δ
5 -2-옥소피페라진 유도체를 고효율 및 고순도로 합성하는 고체상 합성 방법에 관한 것이다.
Δ5-2-옥소피페라진, 유도체, 고체상 합성
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