| 多尼培南的合成 |
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| 引用本文： | 张爱艳,朱雪焱,袁哲东. 多尼培南的合成[J]. 中国医药工业杂志, 2006, 37(6): 361-363 |
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| 作者姓名： | 张爱艳 朱雪焱 袁哲东 |
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| 作者单位： | 上海医药工业研究院,上海,200437 |
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| 摘 要： | 反式-4-羟基-L-脯氨酸经酯化、保护、还原、SN2取代、Mitsunobu反应、醇解得到（2S,4S）-1-叔丁氧羰基-2-（N-叔丁氧羰基氨磺酰胺基）甲基-4-巯基吡咯烷（7）,收率50.8%.7与（1R,5S,6S）-6-[（1R）-1-羟乙基]-2-二苯氧磷酰氧基-1-甲基-1-碳代-2-青霉烯-3-羧酸对硝基苄酯（8）缩合、脱保护,得到多尼培南,收率50.5%（以7计）.总收率接近26%（以反式-4-羟基-L-脯氨酸计）.
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| 关 键 词： | 多尼培南 抗菌剂 合成 |
| 文章编号： | 1001-8255（2006）06-0361-03 |
| 收稿时间： | 2005-12-06 |
| 修稿时间： | 2005-12-06 |
Synthesis of Doripenem |
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| ZHANG Ai-Yan,ZHU Xue-Yan,YUAN Zhe-Dong. Synthesis of Doripenem[J]. , 2006, 37(6): 361-363 |
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| Authors: | ZHANG Ai-Yan ZHU Xue-Yan YUAN Zhe-Dong |
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| Affiliation: | Shanghai Institute of Pharmaceutical Industry, Shanghai 200437 |
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| Abstract: | Doripenem was synthesized by the condensation of (2S,4S) -1-t-butoxycarbonyl-2- (N-t-butoxycarbonyl-sulfamoylamido) methyl-4-mercaptopyrrolidine (7) and (1R,5S,6S) -6- [(1R) -1-hydroxyethyl] -2-diphenoxyphosphonyloxy-l-methyl-l-carba-2-penem-3-carboxylic acid p-nitrobenzylester (8) , followed by deprotection with a yield of 50.5 %. Compound 7 was obtained from trans-4-hydroxy-L-proline by esterificatiom, protection, reduction, SN2 substitution, Mitsunobu reaction and alcoholysis with a yield of 50.8 %. The overall yield was about 26 % (based on trans-4-hydroxy-L-prorine). |
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| Keywords: | doripenem antibacterial synthesis |
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