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Patent Agency Ranking
公开(公告)号：KR1020000051076A
公开(公告)日：2000-08-16
申请号：KR1019990001314
申请日：1999-01-18
Applicant: 한국과학기술연구원
IPC: C07D207/00
Abstract: PURPOSE: Rachlopride derivative attached with an N2S2 ligand useful as imaging compound for a dopamin D2 acceptor and preparing process thereof are provided which label a technetium having the radiochemically optimum physical conditions. CONSTITUTION: A rachlopride derivative represented by the formula (1) is that an N2S2 ligand is introduced into rachlopride to introduce the technetium to the raclopride for the attachment of technetium. The compound has the advantage of labeling a technetium having the optimum physical conditions such as manufacturing easiness, half-life period, radioactive strength and purchase easiness. Also described is a process for preparing the rachlopride.
Abstract translation: 目的：提供与用作多巴胺D2受体的成像化合物的N2S2配体连接的Rachlopride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rachlopride衍生物是将N 2 S 2配体引入rachlopride以将锝引入到raclopride中以连接锝。 该化合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。 还描述了制备rachlopride的方法。
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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：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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