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    • 3. 发明公开
    • N₂S₂ 리간드가 결합된 아릴피페라진 유도체 및 이의 제조방법
    • 与N2S2配体连接的亚苄基衍生物及其制备方法
    • KR1020000051075A
    • 2000-08-16
    • KR1019990001313
    • 1999-01-18
    • 한국과학기술연구원
    • 조정혁오창현이기수유현진이명철정준기이동수정재민
    • C07D211/64
    • 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).
    • 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。
    • 4. 发明公开
    • 파이타제 발현벡터 PJPK 및 이에 의해 형질전환된바실러스 서브틸리스 PJPK.
    • PHYTASE表达载体,PJPK和BACILLUS SUBTILIS PJPK转换
    • KR1020000041160A
    • 2000-07-15
    • KR1019980056952
    • 1998-12-21
    • 주식회사대성미생물연구소한국과학기술연구원
    • 오태광김영옥이정기오병철김동현정준기박승춘김판경최양웅이동규
    • C12N15/63
    • C12N15/63A23K10/16C12N9/14C12R1/125
    • PURPOSE: Phytase expression vector, pJPK has strong BJ27 promoter. Bacillus subtilis pJPK (KCTC 0526BP) transformed with pJPK expresses phytase highly, secrets expressed protein and is nontoxic to animal because of lacking endotoxin such as lipopolysaccharides. CONSTITUTION: Bacillus expression vector pJH27, having strong promoter BJ27, is ligated with 2.2 kb phytase gene originated from Bacillus amyloliquefaciens DS-11. The 2.2kb DNA includes SD sequence of phytase gene complementary to Bacillus subtilis 16S rRNA sequence (UCCUCC) for the overexpression of phytase. Resulting recombinant plasmid, pJPK, is introduced into E. coli JM83. Purified pJPK is transformed into Bacillus subtilis DB104 by protoplast transformation. Modified LB medium is consisted of 1% of potassium phosphate, 0.045% of magnesium sulfate, 4% of glucose, 1% of tryptone, 0.5% of yeast extract, 0.5% of NaCl and trace elements. 500-1000 unit of phytase is added to 1kg of animal feed. Animal experiment with porcine reveals that phytase produced from bacillus effectively degrades phytic acid in the animal feed.
    • 目的:植酸酶表达载体pJPK具有较强的BJ27启动子。 用pJPK转化的枯草芽孢杆菌pJPK(KCTC 0526BP)高度表达植酸酶,秘密表达蛋白质,由于缺乏内毒素,如脂多糖,对动物无毒。 构成:具有强启动子BJ27的芽孢杆菌表达载体pJH27与源自解淀粉芽孢杆菌DS-11的2.2kb植酸酶基因连接。 2.2kb DNA包括与枯草芽孢杆菌16S rRNA序列(UCCUCC)互补的植酸酶基因的SD序列,用于过表达植酸酶。 将得到的重组质粒pJPK导入大肠杆菌JM83中。 纯化的pJPK通过原生质体转化转化到枯草芽孢杆菌DB104中。 改性LB培养基由1%磷酸钾,0.045%硫酸镁,4%葡萄糖,1%胰蛋白胨,0.5%酵母提取物,0.5%NaCl和微量元素组成。 将500-1000单位的植酸酶加入1kg动物饲料中。 猪的动物实验显示,由芽孢杆菌产生的植酸酶有效降解动物饲料中的植酸。
    • 5. 发明公开
    • 메틸렌디포스폰산의제조방법
    • 甲基二磷酸的制备方法
    • KR1020000020033A
    • 2000-04-15
    • KR1019980038443
    • 1998-09-17
    • 한국과학기술연구원
    • 조정혁오창현이기수이창식이명철정준기이동수정재민
    • C07F9/00C07F9/38
    • 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.
    • 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。
    • 8. 发明公开
    • 글루코스 옥시다제의 대량 제조 방법
    • 葡萄糖氧化酶的生产方法
    • KR1020000059736A
    • 2000-10-05
    • KR1019990007559
    • 1999-03-08
    • 한국과학기술연구원
    • 박영훈정준기이홍원
    • C12N15/53C12N15/81
    • C12N9/0004C12N15/81C12R1/685
    • PURPOSE: Provided is a method for mass producing glucose oxidase, from Aspergillus niger by that glucose oxidase is accumulated in high concentration, thereby, purification process is simplified and a production yield is promoted. CONSTITUTION: The mass production method of glucoseoxidase comprises following steps of: preparing an expression plasmid having galactosedehydroginase (GAL10) promoter and galactodehydroginase (GAL7) terminator from yeast, signal sequence and structural gene of Aspergillus niger ATCC-9029; obtaining transformed yeast pJKGo(designation No. KCTC-0581 BP) by introduction of the expression plasmid into Saccharomyces cerevisiae (ATCC-2805); preparing glucose oxidase by the transformed yeast; and then secreting glucose oxidase to outside of cell membrane.
    • 目的:提供从葡萄糖氧化酶以高浓度积累葡萄糖氧化酶的方法,通过葡萄糖氧化酶积累葡萄糖氧化酶,从而简化了纯化过程,提高了产率。 构成:糖酵解酶的大量生产方法包括以下步骤:制备具有半乳糖脱氢酶(GAL10)启动子和来自酵母的半乳糖脱氢酶(GAL7)终止子的表达质粒,黑曲霉ATCC-9029的信号序列和结构基因; 通过将表达质粒引入酿酒酵母(ATCC-2805)中获得转化酵母pJKGo(命名号KCTC-0581BP); 由转化酵母制备葡萄糖氧化酶; 然后将葡萄糖氧化酶分泌到细胞膜外。
    • 9. 发明公开
    • N₂S₂리간드가 결합된 테트라벤아진 유도체 및 그의 제조방법
    • 用N2S2配体连接的四氢萘衍生物及其制备方法
    • KR1020000051077A
    • 2000-08-16
    • KR1019990001315
    • 1999-01-18
    • 한국과학기술연구원
    • 조정혁오창현이기수이창식이명철정준기이동수정재민
    • C07D221/06
    • 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.
    • 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。