| 盐酸他喷他多的合成 |
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| 引用本文： | 马慧,冯文化,梁玉华.盐酸他喷他多的合成[J].中国医药工业杂志,2010,41(9). |
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| 作者姓名： | 马慧 冯文化 梁玉华 |
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| 作者单位： | 北京协和医学院药物研究所,北京,100050 |
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| 摘 要： | 间甲氧基苯丙酮与二甲胺盐酸盐发生Mannich反应生成消旋3-二甲胺基-1-(3-甲氧基苯基)-2-甲基-1-丙酮(13),经结晶诱导的非对映异构体转化得到S-型化合物14后,经格氏反应、酰化及催化氢解得到(2R,3R)-2-甲基3-(3-甲氧基苯基)-N,N-二甲基戊胺,最后经脱保护基、与盐酸成盐得到中枢镇痛药盐酸他喷他多,总收率约52%.
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| 关 键 词： | 他喷他多 中枢镇痛药 阿片μ受体激动剂 肾上腺素能递质摄取抑制剂 结晶诱导 合成 |
Synthesis of Tapentadol Hydrochloride |
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| Authors: | MA Hui FENG Wenhua LIANG Yuhua |
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| Affiliation: | MA Hui,FENG Wenhua,LIANG Yuhua (Institute of Materia Medica Peking Union Medical College,Beijing 100050) |
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| Abstract: | The central analgesics tapentadol hydrochloride was synthesized from 1-(3-methoxyphenyl)-1-propanone by Mannich reaction with dimethylamine hydrochloride to obtain racemic 3-dimethylamino-1-(3-methoxyphenyl)-2-methylpropan-1-one(13),which was subjected to crystallization-induced diastereomer transformation,Grignard reaction,acylation and catalytic hydrogenolysis to give (2R,3R)-2-methyl-3-(3-methoxyphenyl)-N,N-dimethylpentanamine,followed by deprotection and salt formation with an overall yield of about 52%... |
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