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1,3-Acetonedicarboxylic acid와 2,5-dimethoxytetrahydrofuran에 의한 diamine들의 반응에 관한 연구
정대일,송주현,이도훈,이용균,최순규,박유미,한정태,Jung Dai-Il,Song Ju-Hyun,Lee Do-Hun,Lee Yong-Gyun,Choi Soon-Kyu,Park Yu-Mi,Hahn Jung-Tai 한국생명과학회 2006 생명과학회지 Vol.16 No.2
본 연구를 통해 항 경련 활성을 보이는 8-aza-bicyclo[3,2,1]octan-3-one 구조를 모체로 하여 생리활성 및 구조적 특이성을 가진 8-aza-bicyclo[3,2,1]octan-3-one 화합물을 합성하고자 하였다. 본 논문에서는 ethylenediamine 1을 2,5-dimethoxyte-trahydrofuran과 1,3-acetonedicarboxylic acid을 반응시켜 8-(2-pyrrol-1-yl-ethyl)-8-aza-bicyclo[3,2,1]octan-3-one 2(yield ; 5.0%)와 1,2-di-8-aza-bicyclo[3,2,1]octan-3-onyl)ethane 3(yield ; 17.0%)을 합성하였다. 1,3diaminopropane 4의 경우에는, 8-(3-pyrrol-1-yl-propyl)-8-aza-bicyclo[3,2,1]octan-3-one 5(yield ; 6.0%)와 1,3-di-8-aza-bicyclo[3,2,1]octan-3-onyl)propane 6 (yield; 21.0%)을, 그리고 1,8-diaminooctane 7의 경우에는 8-(-8-pyrrol-1-yl-octyl)-8-aza-bicyclo[3,2,1]octan-3-one 8(yield; 2.6%)과 1,8-di-8-aza-bicyclo[3,2,1]octan-3-onyl)octane 9(yield; 24.9%)를 합성할 수 있었다. Diaminoalkanes(1,.4, 7)의 반응에서 보면 실온에서 반응을 진행시켰기에 pyrrole 유도체보다는 8-aza-bicyclo[3,2,1]octan-3-one 유도체의 합성이 보다 유리한 결과를 나타냈다. 그리고 탄소 chain이 길수록 N 원자에 전자를 잘 밀어주어 활성이 더 좋았으며 탄소 steric effect도 작기 때문에 생성물의 yield가 더 높았다. Diaminobenzene(10, 14) 역시 diaminoalkane의 반응과 같이 p-phenylenediamine 10을 2,5-dimethoxytetrahydrofuran, 그리고 1,3-acetonedicarboxylic acid과 반응시켜 p-dipyrrolylbenzene 11(yield; 4.0%), 8-(4-pyrrol-1-yl-phenyl)-8-aza-bicyclo[3,2,1]octan-3-one 12(yield; 12.0%), 1,4-di-(8-aza-bicyclo[3,2,1]octan-3-onyl)-benzene 13(yield; 59.0%)을 합성하였고, m-phynylenediamine 14의 경우에도 8-(3-pyrrol-l-yl-phenyl)-8-aza-bicyclo[3,2,1]octan-3-one 15(yield; 2.0%)와 1,3-di-(8-aza-bicyclo[3,2,1]octan-3-onyl)-benzene 16(yield; 28.0%)을 합성할 수 있었다. 그러나 o-phynylenediamine 17의 경우에는 8-aza-bicyclo[3,2,1]octan-3-one ring들의 steric hindrance의 영향에 의해 1,3-di-8-aza-bicyclo[3,2,1]octan-3-onyl)benzene은 합성되지 않았다. In order to synthesize novel anticonvulsants, we researched that the reactions of diamines with 2,5-dimethoxytetrahydrofuran and 1,3-acetonedicarboxylic acid. The reaction of ethylenediamine with 2,5-dimethoxytetrahydrofuran and 1,3-acetonedicarboxylic acid afforded 8-(2-pyrrol-1-yl-ethyl)-8-aza-bicyclo[3,2,1]octan-3-one (yield; 5.0%) and 1,2-di-(8-aza-bicyclo[3,2,1]octan3-onyl)ethane (yield; 17.0%). In case of 1,3-diaminopropane, 8-(3-pyrrol-1-yl-propyl)-8-aza-bicyclo[3,2,1]octan-3-one(yield; 6.0%) and 1,3-di-(8-aza-bicyclo[3,2,1]octan-3-onyl)propane (yield; 21.0%) were obtained. In case of 1,8-diaminooctane, 8-(8-pyrrol-1-yl-octyl)-8-aza-bicyclo-[3,2,1]octan-3-one (yield; 2.6 %) and 1,8-di-(8-aza-bicyclo[3,2,1]octan-3-onyl)octane (yield; 24.9%) were obtained. In diaminobenzene reactions, synthetic yields of 8-aza-bicyclo-[3,2,1]octan-3-one derivatives were higher than those of pyrrole derivatives because re actions were done under room temperature. The longer the carbon chain of diaminoalkane is, the more reactive N atom is due to more electron donating effect, and the less steric hindrance around the carbon gave the higher chemical yields. The reaction of p-phenylenediamine as a diaminobenzene with 2,5-dimethoxyte-trahydrofuran and 1,3-acetonedicarboxylic acid produced p-dipyrrolylbenzene (yield; 4.0%), 8-(4-pyrrol-1-yl-phenyl)-8-aza-bicyclo[3,2,1]octan-3-one (yield; 12.0%), and 1,4-di-(8-aza-bicyclo[3,2,1]octan-3-onyl)benzene (yield; 59.0%). In case of m-phenylenediamine, 8-(3-pyrrol-1-yl-phenyl)-8-aza-bicyclo[3,2,1]octan-3-one(yield; 2.0%) and 1,3-di-(8-aza-bicyclo[3,2,1]octan-3-onyl)benzene (yield ; 28.0%) were obtained. But, synthesis of 1,2-di-(8-aza-bicyclo[3,2,l]octan-3-onyl)benzene by treatment of o-phenylenediamine was not successful, presumably due to the steric hindrance of 8-aza-bicyclo-[3,2,1]octan-3-one rings.
Synthesis and Activity Evaluation of Imidazolidinetrionylsaccharin Derivatives
정대일,김윤영,김용환,이도훈,이기혜,신여주,김윤혜,변석인,한정태,Jung, Dai-Il,Kim, Yun-Young,Kim, Young-Hwan,Lee, Do-Hun,Lee, Gi-Hye,Shin, Yeo-Ju,Kim, Yun-Hye,Byun, Suk-In,Han, Jung-Tae Korean Society of Life Science 2003 생명과학회지 Vol.13 No.1
새로운 농약을 창출하기 위해, thiazole 유도체 등에서 살균력이 존재하는 구조를 가진 1,2-benzisothiazole-3-one-1,1-dioxide를 선도물질로 imidazolidinetrionyl 기를 가진 새로운 화합물을 합성하였다. 1-methylurea와 oxalyl chloride의 반응으로부터 4단계 반응을 거쳐 1-methyl-3-(1,1,3-trioxo-1,3-dihydro-1λ$^6$-benzo[d]isothiazol-2-ylmethyl) -imidazolidine-2,4,5-triones 5a, 1-ethyl-3- (1,1,3-trioxo-1,3-dihydro-1λ$^6$-benzo[d] isothiazo1-2-ylmethyl)-imidazolidine-2,4,5-triones 5b, 1-phenyl-3-(1,1,3- trioxo-1,3-dihydro-1λ$^6$-benzo[d]isothiazol-2-ylmethyl)-imidazolidine-2,4,5-triones 5c를 합성하였다. 합성된 5a, 5b, 5c를 식물반응, 곤충 그리고 살균제 등에 대한 생물학적 반응검색을 하였다. 생물학적 반응검색 결과(식물반응 검색은 5b, 곤충검색은 5a, 그리고 살균제 검색은 5a에서 생물활성이 조금 나타남) 썩 좋은 반응결과를 얻지 못했다. 하지만 계속해서 2,4,5-imidazolidinetrionyl기를 가진 saccharin유도체를 합성하여 새로운 농약을 창출하고자 한다. 1-Methyl-3-(1,1,3-trioxo-1,3-dihydro-1λ$^6$-benzo[d]isothiazol-2-ylmethyl)-imidazolidine-2,4,5-triones 5a, 1-ethy1-3-(1,1,3-trioxo-1,3-dihydro-lλ$^6$/-benzo[d]isothiazol-2-ylmethyl)-imidazolidine-2,4,5-triones 5b 1-phenyl-3-(1,1,3-trioxo-1,3-dihydro-1λ$^6$-benzo [d]isothiazol-2-ylmethyl)-imidazolidine-2,4,5-triones 5c were obtained by means of 4 reaction steps involved the reaction of 1-methyl-urea and oxalyl chloride. Biological tests(Plant Response Screening Result, Insect Primary Screening Result and Fungicide Primary Screening Result) of synthesized sacccarin derivatives were executed.
Synthesis and Reaction of 1,5,3,7-Diazadiphosphocine-1,5-Dicarboxylic Acids
조승환,송주현,이도훈,이용균,박유미,최순규,한정태,정대일,Cho, Seung-Hwan,Song, Ju-Hyun,Lee, Do-Hun,Lee, Yong-Gyun,Park, Yu-Mi,Choi, Soon-Kyu,Hahn, Jung-Tai,Jung, Dai-Il Korean Society of Life Science 2007 생명과학회지 Vol.17 No.7
본 연구는 MRI 조영제나 새로운 생리활성 물질을 개발키 위해 paraformaldehyde와 hypophosphorous acid를 아미노산인 glycine 혹은 glutamic acid와 함께 반응시켜 3,7-dihydroxy-3,7-dioxoperhydro-1,5,3,7-diazadiphos-phocme-1,5-diacetic acid 1 와 3,7-dihydrexy-3,7-dioxoperhydre-1,5,3,7-diazadiphos-phocme-1,5-di- (2-glutaric acid)3을 합성하였다. 그러나 aspartic acid에 의한 2-[5-(1,2-dicarboxy-ethyl)-3,7-dihydroxy-3,7-dioxo-315.715-[1,5,3,7]diazadiphosphocan-1-yl]-succinic acid 2는 얻지 못했다. 합성 된 3,7-dihydroxy-3,7-dioxoperhydro-1,5,3,7-dia-zadiphosphocine-1,5-diacetic acid 1을 산 촉매에 의한 에스테르화반응시켜 화합물 3,7-dihydroxy-3,7-dioxoper-hydro-1,5,3,7-diazadiphosphocine-1,5-diacetic acid methyl ester 4, 3,7-dihydroxy-3,7-dioxoperhydro-1,5,3,7-dia-zadiphosphocine-1,5-diacetic acid ethyl ester 5, 그리고 3,7-dihyoxy-3,74dioxoperhyo-1,5,3,7-diazadiphosphocine-1,5-diacetic acid propyl ester 6을 합성하였다. 계속해서 다양한 반응을 통해 새로운 화합물을 합성할 것이며 생리활성검색도 실시할 예정이다. In order to synthesize new bioactive compounds and contrasting agents, reactions of glycine and glutamic acid as an animo acid with paraformaldehyde and hypophosphorous acid were executed. Products are 3,7-dihydroxy-3,7-dioxoperhydro-1,5,3,7-diazadiphosphocine-1,5-diacetic acid 1 and 3,7-dihydroxy-3,7- dioxoperhydre-1,5,3,7-diazadiphosphocine-1,5-di-(2-glu taric acid) 3. 2-[5-(1,2-Dicarboxyethyl)-3,7-dihydroxy-3,7-dioxo-315.715-[1,5,3,7] diazadiphosphocan-1-yl]-succinic acid 2 by using aspartic acid was not obtained. Esterification of 3,7- dihydroxy-3,7-dioxoperkydro-1,5,3,7-diaza-diphosphocine-1,5-diacetic acid 1 by treatment of methanol, ethanol, and propanol were executed. 3,7-Dihydroxy-3,7-dioxoperhydro-1,5,3,7-diazadiphosphocine-1,5-diacetic acid methyl ester 4, 3.7-dihydroxy-3,7-dioxoperhydro-1,5,3,f-diazadiphosphocine-1.5-diacetic acid ethyl ester 5, and 3,7-dihydroxy-3,7-dioxoperhydro-1,5,3,7-diazadiphosphocine-1,5-diacetic acid propyl ester 6 were respectively synthesized in good yields. Continuously, we will try synthesis of novel compounds and evaluation of biological activity.
정대일,정선주,김인식,최영하,류정숙,이용균,최순규 동아대학교 환경문제연구소 1999 硏究報告 Vol.22 No.2
The selective absorption ability of low density heavy metal(Pb(Ⅱ) ion or Cu(Ⅱ) ion) of eggshell(raw or boiled) is better than one of existing absorption materials in treatment ability and experimental condition. The elimination ability of chlorine of eggshell(raw or soiled) is worse than one of active carbon. In elimination of trihalomethane, the effect of treatment of eggshell is almost the same as one of pine cones. And surface of eggshell(raw or boiled) after absorption of heavy metal ion was observed by Scanning Electron Microscope(SEM). Application and availability of eggshell(raw or boiled) as absorption material need lots of experiments. The experiment on baked eggshell is proceeding.
Benzodiazepinone들과 Pyridobenzodiazepinone의 합성에 관한 연구
정대일,최순규,박유미,이용균,김윤영,김인식,최태원 東亞大學校附設基礎科學硏究所 1996 基礎科學硏究論文集 Vol.13 No.1
?? 존재하에서 o-phenylenediamine 5와 acrylic acid 11의 반응은 benzodiazepinone 13과 pyridobenzodiazepinone 17을 생성한다. PPA 또는 SiO₂존재하에서의 o-phenylenediamine 5와 acrylic acid 11의 반응은 오직 benzodiazepinone 13만을 생성한다. 100∼110 ℃에서 PPA 또는 ?? 또는 SiO₂존재 하에서 o-phenylenediamine 5와 crotonic acid 19의 반응은 각각 1:1 cycloadduct인 4-methylbenzodiazepinone 20을 얻었다. The reaction of o-phenylenediamine 5 with acrylic acid 11 in the presence of ?? afforded benzodiazepinone 13 and pyridobenzodiazepinone 17. The reactions of o-phenylenediamine 5 with acrylic acid 11 in the presence of PPA or SiO₂afforded only benzodiazepinone 13. The reactions of o-phenylenediamine 5 with crotonic acid 19 in the presence of PPA or ?? or SiO₂at 100∼110℃ afforded respectively 4-methylbenzodiazepinone 20 as 1:1 cycloadduct.