董庆, 刘敦茀. 4-无取代单环β-内酰胺抗生素合成方法的研究J. 药学学报, 1987, 22(1): 19-22.
引用本文: 董庆, 刘敦茀. 4-无取代单环β-内酰胺抗生素合成方法的研究J. 药学学报, 1987, 22(1): 19-22.
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DONG Qing, LIU Dun-Fu. STUDIES ON THE SYNTHETIC METHODS OF 4-UNSUBSTITUTED MONOCYCLIC BETA-LACTAM ANTIBIOTICSJ. Acta Pharmaceutica Sinica, 1987, 22(1): 19-22.
Citation: DONG Qing, LIU Dun-Fu. STUDIES ON THE SYNTHETIC METHODS OF 4-UNSUBSTITUTED MONOCYCLIC BETA-LACTAM ANTIBIOTICSJ. Acta Pharmaceutica Sinica, 1987, 22(1): 19-22.
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4-无取代单环β-内酰胺抗生素合成方法的研究

STUDIES ON THE SYNTHETIC METHODS OF 4-UNSUBSTITUTED MONOCYCLIC BETA-LACTAM ANTIBIOTICS

    摘要
  • 摘要: 本文报道了用L(+)—天门冬氨酸为原料,经Schmidt重排反应得到L(+)-2,3-二氨基丙酸,再在Ph3P—(PyS)2—CH3CN系统中环合得到4-无取代单环β-内酰胺抗生素的关键中间体,N-苄氧甲酰基-3 S-氨基-2-氧吖丁啶(Ⅲ)的方法。研究了用2,2′-二苯并噻唑二硫醚代替(PyS)2作为环合氧化剂;以(Ⅲ)制备了三个新的单环β-内酰胺抗生素衍生物(Ⅷa),(Ⅷb)和(Ⅷc)。

     

    Abstract: The key intermediate of monocyclic beta-lactams, N-benzyloxycarbonyl-3 S-amino-2-oxoazetidine(Ⅲ),was synthesized from L-( + )-2,3-diaminopropanoie acid(Ⅰ) by Ph3P—(PyS)2—CH3CN system and N-benzyloxycarbonylation. Ⅰ was prepared from L(+)-aspartic acid by Schmidt rearrangement.Three derivatives(Ⅷa～c) of this monocyclic beta-lactam were prepared and their biological activities evaluated.

     

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