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β-內醯胺類抗生素的合成和發展

Development and Syntheses on β-Lactam Antibiotics

摘要


β-內醯胺類抗生素為最常應用的第物之一。早期發現的青黴素,芽胞頭素到最新一代的β-內醯胺類抗生素之發展,均已有很多的研究報告。利用酯和亞胺的縮合反應可製備具β-內醯胺環之抗生素。用不對稱性合成法製備高掌性純度的β-內醯胺亦可進一步合成抗生素。利用旋光性化合物如胺基酸或葡萄糖亦可合成此類抗生素。隨著醫藥化學的發達,各類新合成的廣效性β-內醯胺類抗生素也陸續被發展出來。

關鍵字

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並列摘要


β-Lactam antibiotics are one of the most popular medicine. Since the discovery of penicillin and cephalosporin, research on β-lactam chemistry has made considerable progress. Condensations of ester enolates with imines are versatile for achieving the syntheses of β-Iactams. Studies toward asymmetric syntheses of chiral β-lactarns are well developed. Chiral β-Iactarns are useful synthons for the syntheses of carbapenem antibiotics, thienamycin and PS-5. Amino acid and (d)-glucose can be applied to synthesize thienamycin derivatives. Finally, recent development on the new generation of β-lactam antibiotics are discussed.

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