| 4-无取代单环β-内酰胺抗生素合成方法的研究 |
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| 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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| 作者姓名： | 董庆 刘敦茀 |
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| 作者单位： | 四川抗菌素工业研究所 成都
(董庆)，四川抗菌素工业研究所 成都(刘敦茀) |
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| 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)。
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| 关 键 词： | 单环β-内酰胺抗生素 3S-氨基-2-氧吖丁啶 L(+)-2 3-二氨基丙酸 |
| 收稿时间： | 1986-01-05 |
STUDIES ON THE SYNTHETIC METHODS OF 4-UNSUBSTITUTED MONOCYCLIC BETA-LACTAM ANTIBIOTICS |
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| DONG Qing and LIU Dun-Fu.STUDIES ON THE SYNTHETIC METHODS OF 4-UNSUBSTITUTED MONOCYCLIC BETA-LACTAM ANTIBIOTICS[J].Acta Pharmaceutica Sinica,1987,22(1):19-22. |
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| Authors: | DONG Qing and LIU Dun-Fu |
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| 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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| Keywords: | Monocyclic beta-lactam antibiotics 3S-Amino-2-oxo-azetidine L(+)-2 3-Diaminopropanoic acid |
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