| (-)-7-羟基-3-羰基-6-[4-苯氧基-3-羟基-1-(E)-丁烯基]-2-氧杂二环[3,3,0]辛烷合成工艺的改进 |
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| 引用本文： | 王伟,朱红星,陈昌柏. (-)-7-羟基-3-羰基-6-[4-苯氧基-3-羟基-1-(E)-丁烯基]-2-氧杂二环[3,3,0]辛烷合成工艺的改进[J]. 中国药物化学杂志, 2003, 13(4): 224-226 |
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| 作者姓名： | 王伟 朱红星 陈昌柏 |
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| 作者单位： | 天津药物研究院合成一室,天津,300193 |
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| 摘 要： | 目的 改进磺前列酮中间体3(S)-烯醇化合物的合成工艺。方法 以双羟化合物为起始原料经硅醚化、选择性氧化、Wittig-Homer反应、水解及立体还原得到3(S)-烯醇化合物。结果 制备得到目标化合物，总收率11％。结论 改进后的合成方法操作简便、易于掌握、反应条件温和、更加适合工业化生产。
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| 关 键 词： | 药物化学 工艺改进 化学合成 磺前列酮 |
| 文章编号： | 1005-0108(2003)04-0224-03 |
Improvement on the synthetic technology of(-)-7-hydroxy-3-oxo-6-[4-phenoxy-3-hydroxy-1-(E)-butenyl]-2-oxabicyclo[3,3,0]octane |
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| WANG Wei,ZHU Hong-xing,CHEN Chang-bai. Improvement on the synthetic technology of(-)-7-hydroxy-3-oxo-6-[4-phenoxy-3-hydroxy-1-(E)-butenyl]-2-oxabicyclo[3,3,0]octane[J]. Chinese Journal of Medicinal Chemistry, 2003, 13(4): 224-226 |
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| Authors: | WANG Wei ZHU Hong-xing CHEN Chang-bai |
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| Abstract: | Aim To synthesize the title compound,a key intermediate for the synthesis of sulprostone,and modify its synthetic technology. Methods The 3( S )-enol compound was prepared from diols-lactone compound by the trimethylsilyl etherification,selective oxidation,Wittig-Horner reaction,hydrolysis and stereospecific reduction. Results The 3( S )-enol compound was synthesized in the total yield 11%. Conclusion The modified technology is simpler,more moderate and suitable for industrial production. |
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| Keywords: | medicinal chemistry process improvement chemical systhesis sulprostone |
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