-
公开(公告)号：WO2018044130A1
公开(公告)日：2018-03-08
申请号：PCT/KR2017/009629
申请日：2017-09-04
Applicant: 한국과학기술원
Abstract: 본 발명은 특정 위치가 변형된(modified) 목적 단백질의 제조방법에 관한 것으로, 보다 구체적으로는 (a) 목적 단백질의 특정 위치에 아미노산을 첨가하여 변형시킬 위치를 반응기를 가지는 물질로 표지하는 단계; (b) 상기 위치의 표지를 활성화시키는 단계; 및 (c) 상기 활성화된 표지에 번역후변형(post translational modification, PTM) 작용기(moiety)를 부착시켜 변형된 단백질을 수득하는 단계를 포함하는 새로운 탄소-탄소 결합 기반 위치 특이적으로 변형된 목적 단백질의 제조방법에 관한 것이다. 본 발명에 따른 위치 특이적으로 변형된 목적 단백질의 제조 방법은 목적 단백질의 원하는 위치에 원하는 변형(modification)을 추가할 뿐만 아니라, 변형이 추가된 목적 단백질이 세포 내에 존재하는 목적 단백질과 동일한 효과를 나타내어 목적 단백질의 기능연구, 신약 스크리닝에 등에 유용하다.
Abstract translation: 本发明涉及生产在特定位点修饰的靶蛋白质的方法，更具体地涉及生产在特定位置修饰的靶蛋白质的方法， 在一个实施例中， （b）激活该地点的标签; （c）将翻译后修饰（PTM）功能部分连接到活化的标记上以获得修饰的蛋白质，新的基于碳 - 碳键的位点特异性修饰的靶蛋白 及其制造方法。 的根据本发明被改性，以及添加一个变形例（变形例）的兴趣位置的特定的蛋白质的制造方法，期望在靶蛋白的期望位置时，相同的效果所需的蛋白质，该修改的额外靶蛋白是存在于细胞 它对靶蛋白的功能研究，新药的筛选等都很有用。
-
2.发明公开도파민 Ｄ3 및 Ｄ4 수용체의 선택적 활성을 지닌 신규4,5-디히드로이소옥사졸릴알킬피페라진 유도체와, 이의제조방법 失效在DOPAMINE D3和D4受体上具有选择性生物活性的新的4,5-二羟基甲基丙烯酰胺衍生物及其制备方法
公开(公告)号：KR1020020043413A
公开(公告)日：2002-06-10
申请号：KR1020000073122
申请日：2000-12-04
IPC: C07D413/14
CPC classification number: C07D413/04 , C07D261/08
Abstract: PURPOSE: Provided are novel 4,5-dihydroisoxazolylalkylpiperazine derivatives having selective biological activity to dopamine D3 and D4 receptors, and their preparation method by reductive amination in the presence of reductant. CONSTITUTION: 4,5-dihydroisoxazolylalkylpiperazine derivative is represented by the formula(1), wherein R1, R2, R3, R4 and R5 are identical or different from each other, and represents individually hydrogen atom, halogen atom, C1-C6 alkyl group, C1-C6 alkoxy group, C2-C6 alkenyl group, hydroxy group , hydroxymethyl group, aryl group, heteroaryl group, amino group, C1-C6 alkyl amino group, carbonyl group, C3-C8 cycloalkyl group, or C3-C8 heterocyclic group; R6 represents hydrogen atom, halogen atom, alkyl group, C1-C6 alkoxy group, aryl group, pyridyl group, heterocyclic group or pyrimidyl group; X represents CH or nitrogen atom; and n is 3 or 4.
Abstract translation: 目的：提供对多巴胺D3和D4受体具有选择性生物活性的新型4,5-二氢异恶唑烷基哌嗪衍生物及其在还原剂存在下还原胺化的制备方法。 构成：4,5-二氢异恶唑基烷基哌嗪衍生物由式（1）表示，其中R 1，R 2，R 3，R 4和R 5彼此相同或不同，并且表示单独的氢原子，卤素原子，C1-C6烷基， C1-C6烷氧基，C2-C6烯基，羟基，羟甲基，芳基，杂芳基，氨基，C1-C6烷基氨基，羰基，C3-C8环烷基或C3-C8杂环基; R6表示氢原子，卤素原子，烷基，C1-C6烷氧基，芳基，吡啶基，杂环基或嘧啶基; X表示CH或氮原子; n为3或4。
-
-
Patent Agency Ranking
公开(公告)号：KR101369207B1
公开(公告)日：2014-03-04
申请号：KR1020070035685
申请日：2007-04-11
IPC: C07D211/90
Abstract: 본 발명은 이하, "S-(-)-펠로디핀"로 표기되는 S-(-)-에틸메틸 4-(2,3-디클로로페닐)-1,4-디히드로-2,6-디메틸-3,5-피리딘-디카르복실레이트의 제조방법에 관한 것으로서, 키랄성 분리화합물을 포함하는 펠로디핀 유도체를 합성하여 (S)-이성질체를 분리한 후 베타히드록시에스테르의 선택적인 에스테르 교환반응을 통해 S-(-)-펠로디핀을 합성하는 효율적인 제조방법에 관한 것이다. 상기 키랄성 분리물질은 (R)-글리시돌(Glycidol) 또는 (S)-글리시돌로부터 다양한 친핵체와 에폭사이드와의 반응을 통해 합성한다.
(R)-글리시돌, (S)-글리시돌, (S)-(-)-펠로디핀-
公开(公告)号：KR100394086B1
公开(公告)日：2003-08-06
申请号：KR1020000073121
申请日：2000-12-04
IPC: C07D413/14
CPC classification number: C07D413/04 , C07D261/08 , C07D413/14
Abstract: The present invention relates to a novel isoxazolylalkylpiperazine derivatives having selective biological activity at dopamine D3 or D4 receptors represented by the following formula (1), and its preparation method through reductive amination reaction in the presence of reducing agent, wherein R1, R2, R3, R4, R5, R6, X and n are the same as defined in the specification.
Abstract translation: 本发明涉及对下式（1）所示的多巴胺D3或D4受体具有选择性生物活性的新型异恶唑烷基哌嗪衍生物及其在还原剂存在下通过还原胺化反应的制备方法，其中R1，R2，R3， R4，R5，R6，X和n与说明书中的定义相同。
-
6.发明公开
公开(公告)号：KR1020020043918A
公开(公告)日：2002-06-12
申请号：KR1020000073121
申请日：2000-12-04
IPC: C07D413/14
CPC classification number: C07D413/04 , C07D261/08 , C07D413/14
Abstract: PURPOSE: Provided are novel isoxazolylalkylpiperazine derivatives having selective activity for dopamine D3 and D4 receptor represented by the formula(1) and their manufacturing method by reductive amination in the presence of a reductant. The derivatives and their pharmaceutically acceptable salts are useful in the treatment of mental illness. CONSTITUTION: The novel isoxazolylalkylpiperazine derivative of the formula(1) is prepared by reacting amine compound represented by the chemical formula(2) with aldehyde compound shown in the chemical formula(3) in the presence of a reductant selected from NaBH(OAc)3, NaBH3CN and NaBH4 in a reductive amination reaction. In the formulae, R1,R2,R3,R4, and R5 are same or different each other and are hydrogen atom, halogen atom, C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, hydroxy, hydroxymethyl, aryl, heteroaryl, amino group, C1-C6 alkylamino, carbonyl, C3-C8 cycloalkyl, or C3-C8 heterocyclic group; R6 is hydrogen atom, halogen atom, alkyl, C1-C6 alkoxy, aryl, pyridyl, heterocyclic, pyrimidyl group; X is CH or nitrogen atom; and n is 3 or 4.
Abstract translation: 目的：提供具有式（1）表示的多巴胺D3和D4受体选择性活性的新型异恶唑基烷基哌嗪衍生物及其制备方法，在还原胺存在下还原胺化。 衍生物及其药学上可接受的盐可用于治疗精神疾病。 构成：式（1）的新型异恶唑基烷基哌嗪衍生物通过使化学式（2）表示的胺化合物与化学式（3）所示的醛化合物在选自NaBH（OAc）3的还原剂存在下反应来制备 ，NaBH 3 CN和NaBH 4在还原胺化反应中。 在式中，R 1，R 2，R 3，R 4和R 5相同或不同，为氢原子，卤原子，C 1 -C 6烷基，C 1 -C 6烷氧基，C 2 -C 6烯基，羟基，羟甲基，芳基，杂芳基 ，氨基，C1-C6烷基氨基，羰基，C3-C8环烷基或C3-C8杂环基; R6是氢原子，卤素原子，烷基，C1-C6烷氧基，芳基，吡啶基，杂环基，嘧啶基; X是CH或氮原子; n为3或4。
-
公开(公告)号：KR1020080092163A
公开(公告)日：2008-10-15
申请号：KR1020070035685
申请日：2007-04-11
IPC: C07D211/90
Abstract: A method for preparing (S)-(-)-felodipine is provided to synthesize the (S)-(-)-felodipine conveniently from a cheap starting material of (R)- or (S)-glycidol and obtain various intermediates, thereby being applied to asymmetric synthesis of a dihydropyridine compound as well as felodipine. A method for preparing (S)-(-)-felodipine represented by a formula(1) comprises the steps of: (a) after reacting (R)- or (S)-glycidol represented by a formula(2) with dihydropyran(DHP), adding a nucleophile(Nu) thereto to obtain a compound represented by a formula(3); (b) reacting the compound of the formula(3) with di-chitin represented by a formula(4) to obtain a compound represented by a formula(5); (c) reacting the compound of the formula(5) with 2,3-dichlorobenzaldehyde represented by a formula(6) to obtain a compound represented by a formula(7); (d) reacting the compound of the formula(7) with 3-amino-2-butenoate represented by a formula(8) to obtain a felodipine intermediate represented by a formula(9); (e) isolating an (S)-isomer therefrom through recrystallization or silica gel chromatography after treating the felodipine intermediate of the formula(9) with an acid; and (f) subjecting the (S)-isomer to selective esterification to obtain the compound of the formula(1).
Abstract translation: 提供制备（S） - （ - ） - 非洛地平的方法，从（R） - 或（S） - 缩水甘油的廉价原料方便地合成（S） - （ - ） - 非洛地平，并获得各种中间体 适用于二氢吡啶化合物以及非洛地平的不对称合成。 由式（1）表示的（S） - （ - ） - 非洛地平的制备方法包括以下步骤：（a）使由式（2）表示的（R） - 或（S） - 缩水甘油与二氢吡喃 DHP），向其中加入亲核体（Nu），得到式（3）表示的化合物。 （b）使式（3）的化合物与由式（4）表示的二壳多糖反应得到式（5）表示的化合物; （c）使式（5）的化合物与式（6）表示的2,3-二氯苯甲醛反应，得到由式（7）表示的化合物; （d）使式（7）的化合物与由式（8）表示的3-氨基-2-丁烯酸酯反应，得到由式（9）表示的非洛地平中间体; （e）在用酸处理式（9）的非洛地平中间体后，通过重结晶或硅胶色谱分离（S） - 异构体; 和（f）使（S） - 异构体进行选择性酯化，得到式（1）的化合物。
-
8.发明授权도파민 Ｄ3 및 Ｄ4 수용체의 선택적 활성을 지닌 신규4,5-디히드로이소옥사졸릴알킬피페라진 유도체와, 이의제조방법 失效도파민D3및D4체택적택적택적규규,5- ,5- ,5- ,5- ,5- ,5- ,5- ,5- ,5- ,5-규규규규규규규규규규규규규규규규규규규규
公开(公告)号：KR100394083B1
公开(公告)日：2003-08-06
申请号：KR1020000073122
申请日：2000-12-04
IPC: C07D413/14
CPC classification number: C07D413/04 , C07D261/08
Abstract: The present invention relates to 4,5-dihydroisoxazolylalkylpiperazine derivatives having selective biological activity at dopamine D3 and D4 receptors represented by the following Formula (1), and its preparation method through reductive amination reaction in the presence of reducing agent,wherein R1, R2, X and n are the same as defined in the specification.
Abstract translation: 本发明涉及对下式（1）所示的多巴胺D3和D4受体具有选择性生物活性的4,5-二氢异恶唑烷基哌嗪衍生物及其在还原剂存在下通过还原胺化反应的制备方法，其中R1，R2， X和n与说明书中定义的相同。
-
-
-
-
-
-
-
Search Results
8
records
(took 0.023 seconds)
