| 氘标记盐酸苯环壬酯的合成 |
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| 引用本文： | 史卫国,陈家骏,樊士勇,何新华,陈兰福,龚雄麒,仲伯华. 氘标记盐酸苯环壬酯的合成[J]. 同位素, 2011, 24(Z1): 112-115 |
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| 作者姓名： | 史卫国 陈家骏 樊士勇 何新华 陈兰福 龚雄麒 仲伯华 |
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| 作者单位： | 军事医学科学院 毒物药物研究所， 北京100850 |
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| 基金项目： | 国家自然科学基金重大项目分题资助(作用于M受体手性分子的药理学研究203900508);“重大新药创制”国家科技重大专项资助(一类抗晕新药左旋盐酸苯环壬酯的临床研究009ZXJ09004-067) |
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| 摘 要： | 为了开展盐酸苯环壬酯及其光学异构体药代动力学研究，确定代谢途径，进行代谢差异比较，对盐酸苯环壬酯进行了稳定同位素氘标记合成研究。以五氘溴苯为原料，先由格氏反应生成D代中间体α-环戊基-α-D5-苯基羟乙酸乙酯，再经三步反应得到定位标记的盐酸氘代苯环壬酯。该合成路线简捷，同位素原料易得，引入标记原子的步骤短，反应条件较易控制，氘丰度达99%，经质谱、核磁确证结构与盐酸苯环壬脂一致。
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| 关 键 词： | 氘标记 盐酸苯环壬酯 药物合成 |
Synthesis of Deuterated Phencynondte Hydrochloride |
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| SHI Wei-guo,CHEN Jia-jun,FAN Shi-yong,HE Xin-hua, CHEN Lan-fu,GONG Xiong-qi,ZHONG Bo-hua. Synthesis of Deuterated Phencynondte Hydrochloride[J]. Isotopes, 2011, 24(Z1): 112-115 |
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| Authors: | SHI Wei-guo CHEN Jia-jun FAN Shi-yong HE Xin-hua CHEN Lan-fu GONG Xiong-qi ZHONG Bo-hua |
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| Affiliation: | Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China |
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| Abstract: | The experimental details for the preparation of phencynondte labelled with five deuteriums with high chemical purity and isotopic enrichment were researched.Deuterated intermediate compound α-cyclopentyl-α-D5-phenyl-glycolate was synthesized first by Grignard reaction from bromobenzene-d5,the final product deuterated phencynondte hydrochloride was then prepared through next three steps reaction with excellent chemical purity and isotopic enrichment.D abundance of synthetic deuterated phencynondte hydrochloride was 99%,the compound was identified by MS and 1H-NMR. |
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| Keywords: | deuterium labeling phencynondte hydrochloride,drug synthesis |
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