• Title/Summary/Keyword: 2-amino-3

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Synthesis of Peptides Containing Optically Active 2-Amino-3-Phosphonopropionic Acid (광학 활성 2-Amino-3-Phosphonopropionic Acid의 새로운 합성 방법과 그를 포함하는 펩티드의 합성)

  • Kim Sang Bum;Cho Sung Ki;Han Jeong Sik;Kim Yong Joon;Hong Suk-In
    • Journal of the Korean Chemical Society
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    • v.38 no.7
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    • pp.516-520
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    • 1994
  • New synthetic method of optically active 2-amino-3-phosphonopropionic acid from L-serine was developed and their phosphonotripeptides, phthalylglycylglycyl-2-amino-3-(diethylphosphono)-propionic acid methyl ester and phthalylglycyl-L-phenylalanyl-2-amino-3-(diethylphosphono)propionic acid methyl ester, were synthesized by coupling reaction of amino acids with 2-amino-3-phosphonopropionic acid methyl ester.

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Synthesis of -4,9-Dione Derivatives via Intramolecular Cyclization (분자내 고리화반응에 의한 -4,9-Dione 유도체 합성)

  • 신상희;서명은
    • YAKHAK HOEJI
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    • v.35 no.3
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    • pp.231-235
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    • 1991
  • Compounds of the structure of -4,9-dione are known to have an antibacterial activity against Gram-positive bacteria. New kinds of 2-amino-$\alpha$-cyano-$\alpha$-ethoxycarbonyl-niethyl)-1,4-naphthoquino ne was reacted with some alkylamines(methylamine, ethylamine, ethanolarnine, isopropylamine, cyclohexylamine, benzylamine) to yield 2-amino-3-ethoxycarbonyl-N-alkyl-4,9-diones.

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Synthesis and Antitumor Evaluation of N-Alkyl-N-Nitrosocarbamoyl-$\alpha$-Amino- and 3$\beta$-Amino-$\alpha$-Cholestane Derivatives (N-Alkyl-N-Nitrosocarbamoyl-3$\alpha$-Amino-와 3$\beta$-Amino-5$\alpha$-Cholestane 유도체들의 합성 및 항암작용 평가)

  • 김정균;최순규;조인섭;유동식;유성호;문경호
    • YAKHAK HOEJI
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    • v.29 no.2
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    • pp.62-69
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    • 1985
  • The isomeric intermediates, $3{\alpha}$and $3{\beta}-amino-5{\alpha}-cholestane required for the synthesis of N-nitrosoureas, N-(2-chloroethyl)-N-nitrosocarbamoyl-$3{\alpha}-amino-5{\alpha}$-cholestane (9), N-methyl-N-nitrosocarbamoyl-3${\alpha}-amino-5{\alpha}-cholestane$ (10), N-(2-chloroethyl)-N-nitrosocarbamoyl-$3{\beta}-amino-5{\alpha}-cholestane$: (7), and N-methyl-N-nitrosocarbamoyl-$3{\beta}-amino-5{\alpha}-cholestane$ (8) were obtained through the $LiAlH_{4}$ reduction of $5{\alpha}$-cholestan-3-one oxime, followed by the chromatographic separation: the assignment of the stereochemistry of both isomers were based on the shape and chemical shift of $C_{3}$-proton resonances on their NMR spectra and on the elution mobility on the TLC. The urea intermediates, N-(2-chloroethyl) carbamoyl-3.alpha.-amino-5.alpha.-cholestane (13), N-methylcarbamoyl-$3{\alpha}-amino-5{\alpha}-cholestane$ (14), N-(2-chloroethyl) carbamoyl-$3{\beta}-amino-5{\alpha}-cholestane (11) and N-methyl-$3{\beta}-amino-5{\alpha}$-cholestane (12) were prepared by the treatment of each isomers ($3{\alpha}$-amino-and $3{\beta}-amino-5{\alpha}$-cholestane) with alkyl isocyanates in anhydrous $CHCl_{3}$, and the corresponding nitrosoureas, 7-10 were obtained by the nitrosation of the ureas, 11-14, with AcOH (or HCOOH)/$NaNO_{2}$ in ice-cold condition. The inhibitory activity of the nitrosoureas, 7-10, and their intermediates, 12-14 towards the growth of L1210 murine leukemia cells, were examined. Among them, the compounds 9 and 10 exhibited high activity having $ED_{50}$ to be 5.5g/ml and 6.1g/ml, respectively.

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Synthesis of New 2-Amino-4-methylcyano-5-methylsulfonylpyrimidine Derivatives (새로운 2-Amino-4-methylcyano-5-methylsulfonylpyrimidine 유도체들의 합성)

  • Kim, Jung-Hwan;Han, Mun-Su;Kim, Un-Ju
    • Journal of the Korean Chemical Society
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    • v.39 no.9
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    • pp.728-733
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    • 1995
  • The derivatives of 2-amino-4-methylcyano-5-methylsulfonylpyrimidine 6 containing chloro, methoxy, ethoxy, phenoxy, amino and anilino groups at 6-position on the pyrimidine ring were prepared from 2-amino-4-chloro-5-methylsulfonylpyrimidine derivatives 4 and tert-butylcyanoacetate. The derivatives of 2-amino-4-chloro-5-methylsulfonylpyrimidine 4 containing methoxy, ethoxy, isopropoxy, phenoxy, amino and anilino groups at 6-position on the pyrimidine ring were prepared from 2-amino-4,6-dichloro-5-methylsulfonylpyrimidine 3.

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A Convenient Preparation of Polychloroanisidine and Fluorochloroanisole Derivatives (Polychloroanisidine 및 Fluorochloroanisole 유도체의 간편한 합성)

  • Kim, Yu Seon;Kim, Tae Yeong;Kim, Yun Hui
    • Journal of the Korean Chemical Society
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    • v.18 no.4
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    • pp.278-288
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    • 1974
  • Starting from p-dichlorobenzene, 2-amino-4-chloroanisole could be prepared via a nitration, a methoxylation, and subsequent reduction. The repeated chlorination of 2-amino-4-chloroanisole resulted 2-amino-3,4,5-trichloroanisole without any isomeric products. The chlorination of 4-chloro-2-nitroanisole could easily give 2,4-dichloro-6-nitroanisole but polychlorination of the product could not be achieved at the atmospherical pressure. The repeated chlorination of 2-amino-4,6-dichloroanisole could give 2-amino-3,4,5,6-tetrachloroanisole, The Schiemann reaction of 2-amino-4-chloroanisole and 2-amino-4,6-dichloroanisole could give 2-fluoro-4-chloroanisole and 2-fluoro-4,6-dichloroanisole, respectively. The repeated chlorination of these fluorochloroanisoles could give 2-fluoro-3,4,5,6-tetrachloroanisole. In each chlorination process, the components of products were examined by means of NMR spectrometry and the chlorination reaction was repeated without isolating each isomeric product. The feasibility of the present routes of preparations was discussed in respects to the conveniency of reaction conditions and respective overall yields of the processes.

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Effect of 9-Amino-1, 2, 3, 4-tetrahydroacridine on $CCl_4$-Induced Liver Injury in Rats (흰쥐의 사염화탄소로 유도된 간손상에 미치는 9-Amino-1, 2, 3, 4-tetrahydroacridine의 영향)

  • Shin Hea-Soon;Cho Eun-Jung
    • Environmental Analysis Health and Toxicology
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    • v.21 no.1 s.52
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    • pp.87-92
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    • 2006
  • This study was done to investigate the protective effect of novel 9-amino-1, 2, 3, 4-tetrahydroacridine derivatives on the hepatoprotective effect intoxicated rats induced by carbon tetrachloride ($CCl_4$). A series of currently derivatives of 9-amino-1, 2, 3, 4-tetrahydroacridine have been prepared through the alkly substitution or the ring expansion for the treatment of the Alzheimer's disease. The activities of aminotransferase (aspartate and alanine) and contents of alkaline phosphatase, triglyceride and glutathione S-transferase in 9-amino-1, 2, 3, 4-tetrahydroacridine derivatives pretreated rats were significantly decreased compared to the only carbon tetrachloride treated rats but the contents of cholesterol were increased compared to the only $CCl_4$ treated rats. The result indicated that 9-amino-1, 2, 3, 4-tetrahydroacridine derivatives showed hepatoprotective effect in $CCl_4$ treated rats.

Isolation and Characterization of 5,6-Dimethoxy-1,2,3,4-tetrahydro-2(1H)-naphthalenone from Catalytic Reductions of the Respective 2-Amino-, and 2-Nitro-3,4-dihydro-5,6-dimethoxy-1(2H)-naphthalenone (2-Amino-와 2-Nitro-3,4-dihydro-5,6-dimethoxy-1(2H)-naphthalenone의 촉매수소화에서 5,6-Dimethoxy-1,2,3,4-tetrahydro-2(1H)-naphthalenone의 분리 및 구조결정)

  • Kim Jack C.
    • Journal of the Korean Chemical Society
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    • v.23 no.2
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    • pp.94-98
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    • 1979
  • From the catalytic reductions of the respective 2-amino-, and 2-nitro-3,4-dihydro-5,6-dimethoxy-1(2H)-naphthalenone, a major reduction product of 2-amino-5,6-dimethoxy-1,2,3,4-tetrahydro-naphthalene was obtained, along with a minute amount of rearranged product, 5,6-dimethoxy-1,2,3,4-tetrahydro-2(1H)-naphthalenone. The unusual formation of 5,6-dimethoxy-1,2,3,4-tetrahydro-2(1H)-naphthalenone was verified on the basis of ir, and nmr spectra, and elemental analysis. A plausible mechanism for the rearrangement is proposed.

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