• Title/Summary/Keyword: deformylation

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Synthetic Method of Aspartame via Oxidative Deformylation of N-Formyl Aspartame (N-포밀 아스파르테임의 산화 탈포밀 반응에 의한 아스파르테임의 제조 방법)

  • Park, Dong-Hyun;Lee, Yoon-Sik
    • Applied Chemistry for Engineering
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    • v.1 no.1
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    • pp.91-99
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    • 1990
  • For-${\alpha}$-APM was efficiently prepared by the reaction of For-Asp anhydride and Phe-OMe in methylethylketone, $CH_3CN$, and in water. The selective recovery of For-${\alpha}$-APM from the resulting For-${\alpha}$-APM and For-${\beta}$-APM mixture was possible via repetitive extraction at constant pH of 4.00. The oxidative deformylation was successfully performed by using several oxidants including $H_2_O2$/THF, sodium percarbonate, and $H_2_O2$/HCl/MeOH giving APM in high yields. The efficiency of the oxidative deformylation was raised in acidic condition for all the deformylation reactions.

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Synthesis and Biological Activity of 3 - (Substituted) Tetrazolylmethyl Cephalosporins (3- (치환) 테트라조일메칠세파로스포린의 합성과 생리활성)

  • Ko, Ok-Hyun;Kim, Young-Soo;Ko, Bong-Suk;Lee, Jae-Young;Ha, Jai-Chun;Bang, Hee-Jae;Yoo, Jin-Cheol;Kang, Hyung-Ryong
    • YAKHAK HOEJI
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    • v.42 no.1
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    • pp.12-24
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    • 1998
  • For the development of new cephalosporin antibiotics with aminothiazolcarboxymethylethoxyimino moiety on the C-7 position and tetrazolymethyl moiety on the C-3 position of cephe m ring, 7${\beta}$-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxyimino)acetamido]-3-[5-(substituted)tetrazol-2-yl]methyl-3-cephem-4-carboxylic acids(28-35) were synthesized. These compounds were tested for antimicrobial activity in vitro against Gram(+) and Gram(-) bacteria. They showed remarkable antibacterial activity against Escherichia coli AB 1157, Escherichia coli AB 0111, Escherichia coli BE 1186, Micrococcus luteus ATCC 9341, Salmonella typhimurium TV 119, Salmonella typhimurium SL 1102, Staphylococcus aureus IFO 12732, Staphylococcus aureus R-209, but these compounds were not active against Pseudomonas aeruginosa N-10.

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