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Environmentally Benign Large-Scale Synthesis of a Precursor to Vortioxetine
Synthesis ( IF 2.2 ) Pub Date : 2020-05-27 , DOI: 10.1055/s-0040-1707823 John K. Gallos 1 , Stavroula A. Zisopoulou 1 , Anastasia E. Pafili 1 , Petros Gkizis 2 , Thanos Andreou 2 , Theoharis V. Koftis 2 , Alexandra Lithadioti 2 , Efstratios Neokosmidis 2
Synthesis ( IF 2.2 ) Pub Date : 2020-05-27 , DOI: 10.1055/s-0040-1707823 John K. Gallos 1 , Stavroula A. Zisopoulou 1 , Anastasia E. Pafili 1 , Petros Gkizis 2 , Thanos Andreou 2 , Theoharis V. Koftis 2 , Alexandra Lithadioti 2 , Efstratios Neokosmidis 2
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An eco-friendly, high-yielding, and transition-metal-free synthesis of 2-[(2,4-dimethylphenyl)thio]aniline precursor to vortioxetine is reported. Vortioxetine, a multi-modal acting drug with high affinity for a range of serotonergic targets, is used for the treatment of major depressive disorder (MDD). The synthesis – applicable in multi-gram scale – involves the reaction of bis(2,4-dimethyl)iodonium bromide with commercial 2-aminophenyl disulfide, whereas its reaction with 2-aminothiophenol afforded the same product but in low to moderate yields. This method works equally well in deep eutectic solvents (DESs), based on choline chloride (ChCl).
中文翻译：
苯妥西汀的前体的环境友好大规模合成
据报道，沃洛西汀是一种环保型，高产，无过渡金属的2-[（（2,4-二甲基苯基）硫代]苯胺苯胺前体。Vortioxetine是一种对多种血清素能靶标具有高亲和力的多模式药物，用于治疗重度抑郁症（MDD）。合成（以克为单位）适用于溴化双（2,4-二甲基）碘鎓与商业化的2-氨基苯基二硫化物的反应，而其与2-氨基硫酚的反应可提供相同的产物，但收率低至中等。该方法在基于氯化胆碱（ChCl）的深共熔溶剂（DES）中同样有效。
更新日期：2020-05-27
中文翻译：
苯妥西汀的前体的环境友好大规模合成
据报道，沃洛西汀是一种环保型，高产，无过渡金属的2-[（（2,4-二甲基苯基）硫代]苯胺苯胺前体。Vortioxetine是一种对多种血清素能靶标具有高亲和力的多模式药物，用于治疗重度抑郁症（MDD）。合成（以克为单位）适用于溴化双（2,4-二甲基）碘鎓与商业化的2-氨基苯基二硫化物的反应，而其与2-氨基硫酚的反应可提供相同的产物，但收率低至中等。该方法在基于氯化胆碱（ChCl）的深共熔溶剂（DES）中同样有效。
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