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2-Aminobenzamide로부터 Quinazoline-4-one 유도체의 합성(I) -알데히드 및 케톤류와의 반응-
서명은 대한약학회 1985 약학회지 Vol.29 No.2
Reaction between 2-aminobenzamide and thionylchloride gave benzo-2-this-1,3[2H]-diazine-4-one-2-oxide (I) at room temperature. With other carbonyl derivatives quinazoline-4-one derivatives (II-VIII) were obtained.
X-Ray 단결정체 분석에 의한 6,7-디클로로퀴놀린-5,8-디온의 친핵치환반응
서명은,George, Clifford 梨花女子大學校 藥學硏究所 1997 藥學硏究論文集 Vol.- No.6
The compound of the 6.7-dichloroquinoline-5.8-dione has two asymmetric chloro radicals at the position of the C6 and C7. When the compound reacts with ethyl acetoacetate in the presence of sodium ethoxide, it is considered that the C6 and/or C7 position of the compound can be substitued. The exact substitued position of the product (Ⅰ) could not be identified by the NMR analysis in our experiment. Therefore, we synthesized the 3-ethoxycarbonyl-2-methyl-1-N-propyl pyridino (2,3f)indole-4,9-dione by reaction of the product (Ⅰ) with propylamine via intramolecular cyclization to identify the substitued position of the product (Ⅰ) using the X-ray crystallographic structure analysis. The result demonstrates that the the position of nucleophilic substitution of the product (Ⅰ) is at the position of the C6.
Computer Graphics/Grid-Search 분석에 의한 Quinolone Conformation에 관한 이론적 연구
서명은,Suh, Myung-Eun 대한약학회 1994 약학회지 Vol.38 No.6
According to computer graphics/Grid search analysis, ${\beta}-keto$ carboxylic acid of nalidixic acid which has an antibacterial activity as DNA-gyrase inhibitor has been known to have got four different conformational energy values. In orders, the energy value of conformation A,B,C and D was -6.603, -4.114, -1.766 and 7.327 kcal/mol. The difference of energy value between conformation A and D was 13.9 kcal/mol. Usually conformation C was used in literature. However, it had a energy value of -1.766 kcal/mol as the result of the analysis which is about 5 kcal/mol higher than the most stable conformation A. Therefore, conformation A is expected to be more stable than conformation C.
1N-아릴-2-메틸-3-에톡시카르보닐-피리디노 [2,3-f]인돌-4,9-디온 유도체 합성 (Ⅱ)
서명은,박희경 梨花女子大學校 藥學硏究所 1998 藥學硏究論文集 Vol.- No.7
The 6,7-dichloroquinoline-5,8-dione (Ⅰ) was reacted with ethyl acetoacetate in the presence of sodium ethoxide to yield 6-(α-acetyl-α-ethoxycarbonyl methyl)-7-chloro-quinoline-5,8-dione(Ⅱ).When this compound Ⅱ was reacted with some arylamine (phenyl. p-toluyl. p-fluorophenyl. p-chloro-phenyl. p-bromophenyl. p-iodophenyl. p-trifluoromethylphenyl. p-dimethylaminophenyl.indanyl). 1N-aryl-2-methyl-3-ethoxycarbonyl pyridino[2,3-f]-indole-4,9-dione(Ⅲa-i) were obtained via intramolecular cyclization.
서명은,김혜경,김중협 대한약학회 1987 약학회지 Vol.31 No.5
8-tert-Butyl-6,7-dihydro-5-methyl-8H-pyrrolo [3,2-e]-s-triazolo [1,5-a] pyrimidine (Bumepidil), one of the s-triazolo [1,5-a] pyrimidine derivatives, has been recently found to be the most promising potential coronary vasodilator and antihypertensive agent. In this report, a new synthetic approach for Bumepidil, via direct N-amination of amino pyrimidine intermediate, was studied and found to be useful method. The novel synthetic method comprise the following steps, acylation of $\gamma$-butyrolactone, condensation with guanidine, direct N-amination, cyclization, chlorination, and finally cyclization using tert-butyl amine.
2(2', 2'-디에톡시에틸) 아미노벤즈아마이드의 고리화반응 (I)
서명은 대한약학회 1987 약학회지 Vol.31 No.6
1, 4-Benzodiazepin 5-one was prepared from 2-aminobenzamide derivatives by acid catalyzed intermolecular cyclization. N-Alkylation of 2-aminobenzamide with $\alpha$-bromo acetaldehyde diethylacetal to 2(2', 2'-diethoxyethyl) aminobenzamide (I) and subsequent treatment of I with acid gave 1, 4-benzdiazepin 5-one, where as the acetyl derivatives of I did not react to 1, 4-benzodiazepin 5-one but to methyl 4-quinazolone (IV).