[关键词]
[摘要]
合成罗替戈汀关键手性中间体S(?)2-(N-正丙基)胺基-5-甲氧基四氢萘。方法 以5-甲氧基-2-四氢萘酮为起始物,经过正丙胺胺化、10%钯炭催化氢化还原、手性拆分3个步骤合成得到该中间体。结果 手性中间体S(?)2-(N-正丙基)胺基-5-甲氧基四氢萘的总收率为21.5%。结论 该路线的原料廉价易得、收率高,适合罗替戈汀的关键手性中间体S(?)2-(N-正丙基)胺基-5-甲氧基四氢萘的工业化生产。
[Key word]
[Abstract]
To synthesize S(?)2-(N-propylamino)-5-methoxytetralin, the key chiral intermediate of rotigotine. Methods 5-Methoxy-2-tetralone was used as the starting material, amination with propylamine, catalytic hydrogenation by 10% palladium carbon, and chiral separation were carried out and the key chiral intermediate was obtained. Results The overall yield of S(?)2-(N-propylamino)-5-methoxytetralin was 21.5%. Conclusion The synthetic route and the key chiral intermediate of rotigotin have the characteristics of inexpensive, high yield, and suitable for industrial production of S(?)2-(N-propylamino)-5-methoxytetralin.
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[基金项目]
天津市科技支撑计划项目(08ZCKFSH01000)