首页> 外国专利> OPTICALLY ACTIVE 1-(4-NITROPHENYL)-4-METHYL-7,8-METHYLENEDIOXY-3,4-DIHYDRO-5H-2,3-BENZODIAZEPINE AND PROCESS FOR PREPARING SAME

OPTICALLY ACTIVE 1-(4-NITROPHENYL)-4-METHYL-7,8-METHYLENEDIOXY-3,4-DIHYDRO-5H-2,3-BENZODIAZEPINE AND PROCESS FOR PREPARING SAME

机译:光学活性的1-(4-硝基苯基)-4-甲基-7,8-甲基二乙氧基-3,4-二氢-5H-2,3-苯并二氮杂AND及其制备方法

摘要

The invention relates to the (+)- and (-)-enantiomers of the compounds of formula (I) as well as a process for the preparation of these enantiomers. This process comprises reducing 1-(4-nitrophenyl)-4-methyl-7,8-methylenedioxy-5H^_-2,3-benzodiazepine of formula (II) by using an adduct formed from an (R)- or (S)-, respectively, 2-amino-1,1-diphenyl-alkan-1-ol derivative of general formula (III), wherein R1 and R2, which are different, stand for a straight or branched chain C1-4 alkyl group or an unsubstituted phenyl or benzyl group, with one molar equivalent of borane or a borane complex. The enantiomers of the compound of formula (I) are valuable intermediates in the synthesis of therapeutically active compounds.
机译:本发明涉及式(I)化合物的(+)-和(-)-对映体,以及制备这些对映体的方法。该方法包括通过使用由(R)-或(S)形成的加合物还原式(II)的1-(4-硝基苯基)-4-甲基-7,8-亚甲基二氧基-5H ^ -2,3-苯并二氮杂pine )-分别为通式(III)的2-氨基-1,1-二苯基-烷-1-醇衍生物,其中R1和R2不同,代表直链或支链C1-4烷基或未取代的苯基或苄基,具有一摩尔当量的硼烷或硼烷配合物。式(I)化合物的对映异构体是治疗活性化合物合成中的有价值的中间体。

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