摘要
采用两种新选择性保护方法由L-丝氨酸和α-酮戊二酸为原料经几步合成了8个目标化合物。体外抑菌该验表明除TMV外,对金葡球菌209P和大肠杆菌44822具有中等到强的活性。
Two new selective protection synthetic methods were sucessfully studiedin preparations of eight target compounds of 2-[4(S)-4-amido-3-oxo-2-isoxazole]-5-oxo-2-tetrahydrofuran carboxylic acids from 1-serine and alpha-keto-glutaric acid. In one method, unhydrogenizable amido side chains were used as selective protective agents. In another method, acetylacetone was used as a selective protective agent, to avoid the acidic hydrolysis of p-nitrobenzyl ester in gamma-lactone ring.In both methods, yields were higher, and the by products were less than the reaction reported by the Japanese research groups.Except that of TM-V, the antibacterial activities of other compounds against S. aureus 209P and E. coli 44822 were moderate strength.
出处
《中国抗生素杂志》
CAS
CSCD
北大核心
1990年第5期346-352,共7页
Chinese Journal of Antibiotics
基金
国家教委自然科学基金资助项目
关键词
四氢呋喃甲酸
抑菌活性
选择性保护
Selective protection
2-[4(S]-4-amido-3-oxo-2-isoxazole3-5-oxo-2-tetrahydrofuran carboxylic acids
Antibacterial activity