申请人:KANEKA CORPORATION
公开号:EP1457570A1
公开(公告)日:2004-09-15
The present invention is to efficiently and simply prepare an optically active 7-substituted-2-aminotetralin with industrial advantage.
In the process, a 7-substituted-2-tetralone or its bisulfite adduct is reduced with a microorganism to an optically active 7-substituted-2-tetralol. Then, a sulfonyl group is introduced to the hydroxy group to form an optically active 7-substituted-2-sulfonyloxytetralin. Then, with inversion of the configuration, a nitrogen substituent is introduced using a nitrogen nucleophile to form an optically active 2,7-substituted tetralin. Furthermore, if necessary, the nitrogen substituent is converted into a non-substituted amino group. Thus, an optically active 7-substituted-2-aminotetralin or its salt is prepared.
本发明旨在高效、简单地制备具有工业优势的光学活性 7-取代-2-氨基四氢萘。
在制备过程中,用微生物将 7-取代-2-四氢萘酮或其亚硫酸氢盐加合物还原成具有光学活性的 7-取代-2-四氢萘酚。然后,在羟基上引入磺酰基,形成具有光学活性的 7-取代-2-磺酰氧基四氢萘。然后,在反转构型的情况下,使用氮亲核剂引入一个氮取代基,形成具有光学活性的 2,7-取代四氢萘。此外,如有必要,还可将氮取代基转化为非取代氨基。这样,一种具有光学活性的 7-取代-2-氨基四氢萘或其盐就制备出来了。