合成羅替戈汀關鍵手性中間體S(?)2-(N-正丙基)胺基-5-甲氧基四氫萘。方法 以5-甲氧基-2-四氫萘酮為起始物，經過正丙胺胺化、10%鈀炭催化氫化還原、手性拆分3個步驟合成得到該中間體。結果 手性中間體S(?)2-(N-正丙基)胺基-5-甲氧基四氫萘的總收率為21.5%。結論 該路線的原料廉價易得、收率高，適合羅替戈汀的關鍵手性中間體S(?)2-(N-正丙基)胺基-5-甲氧基四氫萘的工業(yè)化生產。

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.

天津市科技支撐計劃項目（08ZCKFSH01000）