| 氨曲南小单环的合成工艺研究 |
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| 引用本文： | 张宏,邓启华,罗有福. 氨曲南小单环的合成工艺研究[J]. 化学世界, 2009, 50(9) |
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| 作者姓名： | 张宏 邓启华 罗有福 |
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| 作者单位： | 四川大学化工学院,四川,成都,610065 |
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| 摘 要： | 以L-苏氨酸为原料,经酯化,酯氨解,氨基N-Cbz(N-苄氧羰基)保护,羟基甲烷磺酰化,酰胺N-磺酸化,分子内环合反应,还原去氨基保护基共7步反应,得到氨曲南中间体(3S,trans)-3-氨基-4-甲基-2-氧代-1-氮杂环丁烷基磺酸,总收率达48.8%,产品经HPLC检测,纯度98.7%,[α]=-41°(c=1%,H2O)。该工艺具有原料易得,后处理简便,收率高,产品纯度高等特点,适合于工业化生产。
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| 关 键 词： | 氨曲南 L-苏氨酸 中间体 合成 |
Study on the Synthesis of(3S,trans)-3-Amino-4-methyl-2-oxo-1-azacyclobutylsulfonic Acid |
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| ZHANG Hong,DENG Qi-hua,LUO You-fu. Study on the Synthesis of(3S,trans)-3-Amino-4-methyl-2-oxo-1-azacyclobutylsulfonic Acid[J]. Chemical World, 2009, 50(9) |
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| Authors: | ZHANG Hong DENG Qi-hua LUO You-fu |
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| Affiliation: | School of Chemical Engineering;Sichuan University;Sichuan Chengdu 610065;China |
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| Abstract: | Started from L-threonine,azetidine[(3S,trans)-3-amino-4-methyl-2-oxo-1-azacyclobutylsulfonic acid] as intermediate of aztreonam was prepared via esterification,aminolysis of ester,protection of amino group by forming N-Cbz and hydroxy group by forming methanesulfonate,subsequently sulfonation on amino of amide,cyclization,and deprotection.The overall yield was 48.8%,and the purity was 98.7%(HPLC),[α]=-41°(c 1%,H_2O).The process had merits such as available raw materials,simple work-ups,highly yield and purity,and it was suitable for industrial production. |
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| Keywords: | aztreonam L-threonine intermediate synthesis |
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