| 替加环素的合成 |
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| 引用本文： | 刘帅,姚颖,李子成,张会.替加环素的合成[J].中国医药工业杂志,2011,42(4). |
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| 作者姓名： | 刘帅 姚颖 李子成 张会 |
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| 作者单位： | 1. 四川大学化学工程学院,四川,成都,610065
2. 成都百裕科技制药有限公司,四川,成都,611130 |
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| 摘 要： | 盐酸米诺环素经硝化和还原得9-氨基米诺环素二硫酸盐(8),经盐酸和氨水处理得9-氨基米诺环素盐酸盐(9);另以溴乙酸叔丁酯为原料,经缩合、酸水解和氯化得N-叔丁基甘氨酰氯盐酸盐(5).5和,反应后经乙醇-丙酮(1:1)及丁醇重结晶,制得抗生素替加环素,总收率约28%(以盐酸米诺环素计),纯度99.8%.
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| 关 键 词： | 替加环素 抗生素 合成 |
Synthesis of Tigecycline |
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| Authors: | LIU Shuai YAO Ying LI Zicheng ZHANG Hui |
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| Institution: | LIU Shuai1,YAO Ying1,LI Zicheng1,ZHANG Hui2(1.School of Chemical Engineering,Sichuan University,Chengdu 610065,2.Chengdu Baiyu Pharmaceutical Co.,Ltd.,Chengdu 611130) |
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| Abstract: | 9-Aminominocycline disulfate(8) was synthesized from minocycline hydrochloride by nitration and reduction.Compound 8 was treated with hydrochloric acid and ammonium hydroxide to form 9-aminominocycline hydrochloride(9).N-t-Butylglycyl chloride hydrochloride(5) was prepared from butyl 2-bromoacetate through condensation,acid hydrolysis and chlorination.Tigecycline was synthesized from condensation of compound 9 with 5,and recrystallization with ethanol-acetone(1:1) followed by butanol.The overall yield was a... |
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| Keywords: | tigecycline antibiotics synthesis |
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