首页> 外国专利> PROCESS FOR PREPARING OPTICALLY ACTIVE 2-CHLOR-12-SQUARE BRACKETS OPEN 3-/DIMETHYLAMINO/-2-METHYLPROPYL SQUARE BRACKETS CLOSED -12H-DIBENZO /ALPHA, G/ /1,3,6/ DIOXIZOLINE

PROCESS FOR PREPARING OPTICALLY ACTIVE 2-CHLOR-12-SQUARE BRACKETS OPEN 3-/DIMETHYLAMINO/-2-METHYLPROPYL SQUARE BRACKETS CLOSED -12H-DIBENZO /ALPHA, G/ /1,3,6/ DIOXIZOLINE

机译:制备光学活性的2色12色方括号的方法开放的3- /二甲基氨基/ -2-甲基丙烯基方括号的方法-12H-二苯并/ Alpha,G / / 1,3,6 /二恶唑啉

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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