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公开(公告)号：KR100275792B1
公开(公告)日：2000-12-15
申请号：KR1019980038442
申请日：1998-09-17
Applicant: 한국과학기술연구원
IPC: C07C321/04
Abstract: 본발명은 신규의 지방산 유도체, 즉 15-메르캅토-3-메틸-펜타데칸산 및 그의 제조방법에 관한 것으로서, 15-메르캅토-3-메틸-펜타데칸산의 테크네슘(Technetium)화합물은 의학 진단용 영상화제로 유용하다.
본 발명의 15-메르캅토-3-메틸-펜타데칸산는 테크네슘과의 표지효율이 우수하고, 테크네슘-화합물은 심장의 β-산화 대사를 조영하는 방사성 의약품으로서 β-메틸기를 가지고 있어 심장에서의 보유기간이 길어 SPECT 등에 유효하다는 장점을 가지고 있다.-
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：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：KR1020000051066A
公开(公告)日：2000-08-16
申请号：KR1019990001304
申请日：1999-01-18
Applicant: 한국과학기술연구원
IPC: C07D487/00
Abstract: PURPOSE: Flumazenil derivatives containing a N2S2 ligand and preparing process thereof are provided which are expected to be useful for imaging benzodiazapine CONSTITUTION: A flumazenil derivatives represented by the formula (1), 2-methyl-1-({2-methyl-2-£(2-methyl-2-sulfanylpropyl)amino|propane-2-thiol, 8-fluoro-3-(hydroxymethyl)-5-methyl-4H-benzo£f|imidazole£1,5-al|1,4-diazaperhydroepine- 6-one are prepared. New compound which is capable of being used as a ligand of technetium, being inexpensive and convenient to handle and having appropriate half-life period is provided by this process when a benzodiazepin acceptor is imaged.
Abstract translation: 目的：提供含有N2S2配体的氟马西尼衍生物及其制备方法，其可用于成像苯并二氮萘成分：由式（1）表示的氟马西尼衍生物，2-甲基-1 - （{2-甲基-2- （2-甲基-2-硫烷基丙基）氨基|丙烷-2-硫醇，8-氟-3-（羟甲基）-5-甲基-4H-苯并咪唑1,2,5-三 当苯并二氮杂受体成像时，通过该方法提供能够用作锝配体的新化合物，其便宜且方便处理并具有适当的半衰期。
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公开(公告)号：KR100299045B1
公开(公告)日：2001-09-22
申请号：KR1019990001313
申请日：1999-01-18
Applicant: 한국과학기술연구원
IPC: C07D211/64
Abstract: 종래의세로토닌수용체영상용화합물의단점을극복하면서 5-HT에대한친화성을높게유지할수 있고방사화학적으로가장최적의물리적조건(제조용이성, 반감기, 방사능세기, 구매용이성)을가지는, 아릴피페라진유도체와 NS리간드의결합에의한티올형화합물을제공하여이에테크네슘을표지할수 있도록한다.
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Patent Agency Ranking
公开(公告)号：KR1020000051075A
公开(公告)日：2000-08-16
申请号：KR1019990001313
申请日：1999-01-18
Applicant: 한국과학기술연구원
IPC: C07D211/64
Abstract: PURPOSE: Arylpiperazine derivatives attached with an N2S2 ligand useful as an imaging compound for serotonin receptors and preparing process thereof are provided which have the advantage of labelling a technetium being free from amide hydrolysis and having high affinity with 5-HT1A. CONSTITUTION: A process for preparing tetrabenazine derivatives represented by the formula (1) comprises the steps of synthesizing arylpiperazine derivatives, synthesizing an N2S2 ligand and attaching the N2S2 ligand to the arylpiperazine derivatives. In formula, X denotes methoxy, trifluoromethyl, or chloro; Y denotes carbon or nitrogen; Z denotes carbon or nitrogen. The compound has the advantage of labeling a technetium having the radiochemically optimum physical conditions(manufacturing easiness, half-life period, radioactive strength and purchase easiness).
Abstract translation: 目的：提供用作用作血清素受体成像化合物的N2S2配体附着的芳基哌嗪衍生物及其制备方法，其具有标记锝不含酰胺水解并且与5-HT1A具有高亲和力的优点。 构成：由式（1）表示的制备丁苯那嗪衍生物的方法包括合成芳基哌嗪衍生物，合成N 2 S 2配体并将N 2 S 2配体连接到芳基哌嗪衍生物的步骤。 在式中，X表示甲氧基，三氟甲基或氯; Y表示碳或氮; Z表示碳或氮。 该化合物具有标记具有放射化学最佳物理条件（制造容易度，半衰期，放射性强度和购买容易度）的锝的优点。
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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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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). -
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