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A HIGHLY STEREOSELECTIVE SYNTHESIS OF SERTRALINE

机译:舍曲林的高度立体选择性合成

摘要

The present invention relates to a process for highly stereoselective synthesis of sertraline and sertraline intermediate. Thus, the mixture of 4-(3,4-Dichlorophenyl)-3,4-dihydro-N-methyl-1(2H)-naphthalenimine, 5% Pd/CaCOSUB3/SUB, water and methanol is taken in a hydrogenation flask and then subjected to hydrogenation under a hydrogen pressure of 0.5 Kg at 20-35° C. for 3 hours 30 minutes. The catalyst is removed by filtration and the solvent is evaporated completely under vacuum to obtain cis-(±)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-naphthalen amine. (trans-(±): 0.2).
机译:本发明涉及用于舍曲林和舍曲林中间体的高度立体选择性合成的方法。因此,4-(3,4-二氯苯基)-3,4-二氢-N-甲基-1(2H)-萘亚胺,5%Pd / CaCO 3 ,水和甲醇的混合物为将其放入氢化烧瓶中,然后在0.5Kg的氢气压力下在20-35℃下氢化3小时30分钟。通过过滤除去催化剂,并在真空下将溶剂完全蒸发,以获得顺式-(±)-4-(3,4-二氯苯基)-1,2,3,4-四氢-N-甲基-萘胺。 (反式-(±):0.2)。

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