首页> 外国专利> Optically active 2 - (chlorine) - 12 - (3 - (dimethylamino) - 2 - (methyl) - propyl) - 12h - dibenzo (d, g) (1,3,6) dioxazocine as well as their acid-addition salts, to processes for their preparation and pharmaceutical compositions containing these compounds

Optically active 2 - (chlorine) - 12 - (3 - (dimethylamino) - 2 - (methyl) - propyl) - 12h - dibenzo (d, g) (1,3,6) dioxazocine as well as their acid-addition salts, to processes for their preparation and pharmaceutical compositions containing these compounds

机译:旋光2-(氯)-12-(3-(二甲氨基)-2-(甲基)-丙基)-12h-二苯并(d,g)(1,3,6)二恶唑啉及其酸加成盐,其制备方法和含有这些化合物的药物组合物

摘要

The invention relates to optically active 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]di oxazocine of the Formula IMAGE (I) and pharmaceutically acceptable acid additional salts thereof. The enantiomers are especially active against Parkinsion's disease. The optically active enantiomers are prepared by (a) resolving the racemic 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]-d ioxazocine with a optically active organic acid and separating the enantiomers; or (b) dissolving the racemic 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]-d ioxazocine in an organic solvent, crystallizing and isolating one of the enantiomers, optionally dissolving additional racemic 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]-d ioxazocine in the mother liquor obtained and crystallizing and isolating the other enantiomer, and, if desired, repeating the whole process.
机译:本发明涉及式(I)的旋光的2-氯-12-(3-二甲基氨基-2-甲基丙基)-12H-二苯并[d,g] [1,3,6]二恶唑啉和药学上可接受的酸的其他盐。对映异构体对帕金森氏病特别有效。通过(a)用光学方法拆分外消旋的2-氯-12-(3-二甲基氨基-2-甲基丙基)-12H-二苯并[d,g] [1,3,6] -d恶唑嗪来制备旋光对映体活性有机酸和分离对映体; (b)将外消旋的2-氯-12-(3-二甲基氨基-2-甲基丙基)-12H-二苯并[d,g] [1,3,6]-二恶唑啉溶解在有机溶剂中,结晶并分离出一种的对映异构体,任选将另外的外消旋的2-氯-12-(3-二甲基氨基-2-甲基丙基)-12H-二苯并[d,g] [1,3,6] -d恶唑嗪溶解于所得母液中,并进行结晶和分离其他对映异构体,并且,如果需要,重复整个过程。

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