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Patent Agency Ranking
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-
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：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：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：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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