| 一种新型噁唑烷酮类抗生素的合成 |
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| 引用本文： | 赵胜贤,厉昆,胡红华,李啸风,任党培,金晓鲁,陈治.一种新型噁唑烷酮类抗生素的合成[J].合成化学,2017,25(3). |
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| 作者姓名： | 赵胜贤 厉昆 胡红华 李啸风 任党培 金晓鲁 陈治 |
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| 作者单位： | 1. 浙江普洛得邦制药有限公司,浙江 东阳 322118;优胜美特制药有限公司,浙江 金华 321025;2. 浙江普洛得邦制药有限公司,浙江 东阳,322118;3. 优胜美特制药有限公司,浙江 金华,321025 |
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| 摘 要： | 以2,4-二溴吡啶为原料,经Weinreb酰胺酰化、Noyori不对称氢转移反应、脱Boc保护基、环化、Suzuki偶联、磷酸单酯化及成盐共七步反应制得一种新型噁唑烷酮类抗生素【【(3R,3aS)-7-{6-(S)3-甲基-2-噁唑烷酮-5-基]吡啶-3-基}-1-氧-1,3,3a,4-四氢苯并b]噁唑3,4-d]1,4]噁嗪-3-基】甲基】磷酸单酯二钠盐,其结构经~1H NMR,~(13)C NMR和HR-MS(ESI)确征,总收率7%,纯度99.7%。
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| 关 键 词： | 2 4-二溴吡啶 磷酸单酯 噁唑烷酮 抗生素 药物合成 |
Synthesis of A Novel Oxazolidinone Antibiotic |
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| ZHAO Sheng-xian,LI Kun,HU Hong-hua,LI Xiao-feng,REN Dang-pei,JIN Xiao-lu,CHEN Zhi.Synthesis of A Novel Oxazolidinone Antibiotic[J].Chinese Journal of Synthetic Chemistry,2017,25(3). |
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| Authors: | ZHAO Sheng-xian LI Kun HU Hong-hua LI Xiao-feng REN Dang-pei JIN Xiao-lu CHEN Zhi |
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| Abstract: | A novel oxazolidinone antibiotic, disodium (3R,3aS)-7-{6-(S)3-methyl-2-oxazolidino-5-yl]pyridin-3-yl}-1-oxo-1,3,3a,4-tetrahydrobenzob]oxazolo3,4-d]1,4]oxazin-3-yl]methyl]phpsphate, was synthesized by seven-step reactions from 2,4-dibromopyridine, via acylation by Weinreb amide, Noyori asymmetric transfer hydrogenation, removal of Boc protecting group, cyclization, Suzuki coupling, mono-phosphate esterfication and salification.The structure was confirmed by 1H NMR, 13C NMR and HR-MS(ESI).The overall yield and purity were 7% and 99.7%, respectively. |
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| Keywords: | 2 4-dibromopyridine mono-phosphate oxazolidinone antibiotic drug synthesis |
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