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Patent Agency Ranking
公开(公告)号：KR1020010077072A
公开(公告)日：2001-08-17
申请号：KR1020000004630
申请日：2000-01-31
Applicant: 한국과학기술연구원
IPC: C07D477/20
Abstract: PURPOSE: Provided are novel 1-β-methylcarbapenem derivatives substituted by pyrrolidine containing imidazoline ring which are strong antibiotics against resistant bacteria. CONSTITUTION: The compound is represented by chemical formula 1, where R is C1-6 low alkyl, aryl and benzyl group which are substituted by one or more groups from hydrogen, hydroxy, amine, sulfonyl and aminosulfonyl group. The process of preparing the compound consists of: converting diazoazetidione compound, chemical formula 2, to two ring keto ester under rhodium acetate catalyst and reacting at 0-5deg.C with diphenylchlorophosphate under base such as diisopropylethylamine; reacting the resultant with thiol derivative of chemical formula 3, and eliminating allyl group from the product by reacting with tributyltinhydride under tetrakisphosphine palladium(0) catalyst at room temp. for 2 hours. After reactions, distilled water is added to extract the water layer and it is freeze dried to get the final compound.
Abstract translation: 目的：提供由吡咯烷咪唑啉环取代的新颖的1-β-甲基碳青霉烯衍生物，它们是抗性细菌的强抗生素。 构成：该化合物由化学式1表示，其中R为被氢，羟基，胺，磺酰基和氨基磺酰基中的一个或多个基团取代的C 1-6低级烷基，芳基和苄基。 制备化合物的方法包括：在乙酸铑催化剂下将二唑并二酮化合物，化学式2转化为两个环酮酯，并在0-5℃与二氯丙酸二苯酯在二异丙基乙胺的碱下反应; 使所得物与化学式3的硫醇衍生物反应，并在室温下在四膦合钯（0）催化剂下与三丁基氢化锡反应从产物中除去烯丙基。 2小时。 反应后，加入蒸馏水提取水层，冷冻干燥，得到最终的化合物。
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公开(公告)号：KR100325375B1
公开(公告)日：2002-03-06
申请号：KR1020000004630
申请日：2000-01-31
Applicant: 한국과학기술연구원
IPC: C07D477/20
Abstract: 본 발명은 다음 화학식 1을 갖는 신규한 카바페넴 유도체 및 그의 제조 방법을 제공한다:
화학식 1
식 중, R은 수소이거나, 하이드록시기, 아민기, 설포닐기 및 아미노설포닐기로 이루어진 군 중에서 선택된 한 가지 이상의 치환기로 치환될 수 있는 C
1∼6 의 저급 알킬기, 알릴기 또는 벤질기이다.-
公开(公告)号：KR1020000051077A
公开(公告)日：2000-08-16
申请号：KR1019990001315
申请日：1999-01-18
Applicant: 한국과학기술연구원
IPC: C07D221/06
Abstract: PURPOSE: Tetrabenazine derivatives attached with an N2S2 ligand useful as an imaging compound for endoplasmic reticulum transporter or reuptake site and preparing process thereof are provided which label a technetium having the radiochemically optimum physical conditions. CONSTITUTION: A tetrabenazine derivatives represented by the formula (1) have the advantage of labelling a technetium having the optimum physical conditions such as manufacturing easiness, half-life period, radioactive strength and purchase easiness. Also the compound can image an endoplasmic reticulum transporter as a marker of Parkinson's disease by attaching an N2S2 ligand to tetrabenazine to introduce technetium into tetrabenazine and providing an imaging compound of the transporter as a radioligand.
Abstract translation: 目的：提供与用作内质网转运体或再摄取位点的成像化合物的N2S2配体连接的丁苯那嗪衍生物及其制备方法，其标记具有放射化学最佳物理条件的锝。 构成：由式（1）表示的丁苯那嗪衍生物具有标记具有制造容易性，半衰期，放射性强度和购买容易性等最佳物理条件的锝的优点。 此外，化合物可以通过将N2S2配体连接到丁苯那嗪来将内质网转运蛋白图像化为帕金森病的标记物，以将锝引入到丁苯那嗪中，并将转运体的成像化合物作为放射性配体提供。
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公开(公告)号：KR100281827B1
公开(公告)日：2001-04-02
申请号：KR1019980038443
申请日：1998-09-17
Applicant: 한국과학기술연구원
Abstract: 본 발명은 유기 아민의 아실화 방법에 있어서, 아실화제로서 다음 화학식 1을 갖는 N,N-디아실이미다졸론 유도체를 사용하는 아실화 방법을 제공한다:
화학식 1.
식 중에서,
R
1 과 R
2 는 같거나 다르고, 메틸, 에틸 또는 C
3 -C
19 의 직쇄 또는 치환된 알킬기, 페닐, 헤테로 사이클릭 화합물, 알콕시기 및 유기산 치환기로 이루어진 군 중에서 선택되며;
R
3 와 R
4 는 같거나 다르고, 수소 원자, 메틸 또는 에틸, 페닐, 치환된 페닐 및 알콕시카보닐기로 이루어진 군 중에서 선택되거나, R
3 와 R
4 는 이들이 결합되어 있는 탄소 원자와 함께 다음 구조를 갖는 R 치환 벤젠 고리를 형성함
(여기서, R은 수소 원자, 카르복실기 또는 설폰산기임).-
公开(公告)号：KR1020000020033A
公开(公告)日：2000-04-15
申请号：KR1019980038443
申请日：1998-09-17
Applicant: 한국과학기술연구원
Abstract: PURPOSE: A preparation method of methylene diphosphonic acid by using diidomethane having a higher boiling point than reaction temperature is provided which produces the title compound in high yield, improves high productivity and is very economic by reusing trialkylphosphate as a starting material. CONSTITUTION: A process is disclosed for preparing methylene diphosphonic acid(1) which comprises: (a)preparing tetralkylmethylenediphosphonic acid ester(4) by reacting trialkyl phosphate(2) with diiodomethane(3); (b)separating the compound(4) from the reactant by removing alkyl iodine; (c)recovering excess trialkylphosphate by distillation at 180°C and recycling to the process(a); (d)removing alkyl groups by thermal-cracking the ester at 200-210°C and recrystallizing. In formula, R is allyl, isopropyl, t-butyl, isobutyl. The compound is useful as raw material of radioactive pharmaceuticals for diagnosis.
Abstract translation: 目的：提供通过使用沸点比反应温度高的二甲基亚甲基二膦酸的制备方法，其以高产率产生标题化合物，提高高生产率，并且通过重复使用三烷基磷酸酯作为起始原料是非常经济的。 公开：制备亚甲基二膦酸（1）的方法，其包括：（a）通过使三烷基磷酸酯（2）与二碘甲烷（3）反应制备四烷基亚甲基二膦酸酯（4）; （b）通过除去烷基碘将化合物（4）与反应物分离; （c）通过在180℃下蒸馏回收过量的三烷基磷酸酯并再循环至方法（a）; （d）通过在200-210℃下热裂解酯并重结晶来除去烷基。 在式中，R是烯丙基，异丙基，叔丁基，异丁基。 该化合物可用作放射性药物的诊断原料。
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