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Patent Agency Ranking
公开(公告)号：KR1020010073625A
公开(公告)日：2001-08-01
申请号：KR1020000002389
申请日：2000-01-19
Applicant: 한국과학기술연구원
IPC: C07D401/12
Abstract: PURPOSE: An arylpiperazine compound and a producing method thereof are provided. The arylpiperazine compound can label technetium and F-18 with no having disadvantages of prior arts. CONSTITUTION: The arylpiperazine compound is represented by formula (1), in which R is methanesulfonyl, paratoluenesulfonyl or trifluoromethanesulfonyl. A compound of formula (1a) is produced by treating a compound of formula (7) with mesyl chloride under triethylamine. A compounds of formula (1b) is produced by reacting a compound of formula (13) with sodium hydrogen and the compound of formula (7) to produce a compound of formula (14); and dissolving the compound of formula (14) in anhydrous anisole and reacting with anhydrous trifluoro acetic acid, in which the compound of formula (13) is produced by dissolving a compound of formula (9) into trifluoro acetic acid and reacting with triphenylmethanol to produce a compound of formula (10); reacting the compound of formula (10) with triethylamine and bromoacetyl bromide to produce a compound of formula (11); reacting the compound of formula (11) with triphenylmethanol under trifluoro acetic acid to produce a compound of formula (12); and reacting the compound of formula (12) with 3-bromopropionyl chloride. The formula (1b), (9) to (14) are described as in the description.
Abstract translation: 目的：提供芳基哌嗪化合物及其制备方法。 芳基哌嗪化合物可以标记锝和F-18，没有现有技术的缺点。 构成：芳基哌嗪化合物由式（1）表示，其中R是甲磺酰基，对甲苯磺酰基或三氟甲磺酰基。 通过在三乙胺下用甲磺酰氯处理式（7）化合物来制备式（1a）化合物。 通过使式（13）化合物与氢钠和式（7）化合物反应制备式（14）化合物来制备式（1b）化合物; 并将式（14）化合物溶于无水苯甲醚中，与无水三氟乙酸反应，其中式（13）化合物通过将式（9）化合物溶解在三氟乙酸中并与三苯基甲醇反应产生 式（10）的化合物; 使式（10）化合物与三乙胺和溴乙酰溴反应生成式（11）化合物; 在三氟乙酸下使式（11）化合物与三苯基甲醇反应，生成式（12）化合物; 并使式（12）化合物与3-溴丙酰氯反应。 公式（1b），（9）〜（14）在说明书中进行说明。
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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.-
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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：KR1020010073626A
公开(公告)日：2001-08-01
申请号：KR1020000002390
申请日：2000-01-19
Applicant: 한국과학기술연구원
IPC: C07D307/00
Abstract: PURPOSE: The benzamide compounds and a producing method thereof are provided, thereby the benzamide compounds can label technesium which is a radioisotope and F-18 with no having disadvantages of prior arts. CONSTITUTION: The benzamide compounds are represented by formula (1), in which R is methanesulfonyl, paratoluenesulfonyl or trifluoromethanesulfonyl. The compound of formula (1a) is produced by dissolving the compound of formula (7) in sulfonyl chloride, neutralizing the solution with sodium sulfate, and removing the solvent to produce the compound of formula (8); dissolving the compound of formula (8) in toluene, dropping thionyl chloride to the solution, removing the solvent by distilling under reduced pressure, dissolving it in organic solvent, and reacting the solution with the compound of formula (6) to produce the compound of formula (9); dissolving the compound of formula (9) in organic solvent and reacting the solution with boron tribromide to produce the compound of formula (10); and dissolving the compound of formula (10) in organic solvent and reacting the solution with methanesulfonyl chloride.
Abstract translation: 目的：提供苯甲酰胺化合物及其制备方法，由此苯甲酰胺化合物可以标记作为放射性同位素的技术和不具有现有技术缺点的F-18。 构成：苯甲酰胺化合物由式（1）表示，其中R是甲磺酰基，对甲苯磺酰基或三氟甲磺酰基。 式（1a）化合物通过将式（7）化合物溶解在磺酰氯中，用硫酸钠中和溶液并除去溶剂以制备式（8）化合物来制备。 将式（8）化合物溶于甲苯中，将亚硫酰氯滴加至溶液中，通过减压蒸馏除去溶剂，将其溶解在有机溶剂中，并使该溶液与式（6）化合物反应，生成 公式（9）; 将式（9）化合物溶解在有机溶剂中，并使该溶液与三溴化硼反应，生成式（10）化合物; 并将式（10）的化合物溶于有机溶剂中，并使该溶液与甲磺酰氯反应。
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