CAS: 43200-83-5; 3-((5-Chloropyridin-2-yl)Carbamoyl)Pyrazine-2-Carboxylic Acid

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5-chloro-2-pyridylamine 2,3-pyrazinedicarboxylic anhydride 6-(5-chloro-2-pyridyl)-5,7-dioxo-6,7-dihydro-5H-pyrrolo(3,4-b)pyrazine N-{4-[(2-{[tert-butyl(dimethyl)silyl]oxy}ethyl)amino]phenyl}-N'-(5-chloropyridin-2-yl)pyrazine-2,3-dicarboxamide (R)-6-(5-chloropyridin-2-yl)-7-oxo-6,7-dihydro-5H-pyrrolo[3,4b]pyrazin-5-yl 4-methylpiperazine-1-carboxylate D-(+)-O,O'-dibenzoyltartaric acid salt eszopiclone dibenzoyl-D-tartrate

📜2-氨基-5-氯吡啶,2,3-吡嗪二酸酐 以in Resulting The Product,3-(5-Chloropyrid-2-yl)Carbamoyl-Pyrazine-2-Carboxylic Acid (Iii)的收率获得产物3-(5-氯-吡啶-2-基氨基甲酰基)-吡嗪-2-羧酸
参考文献:Process For The Preparation Of Eszopiclone
标题:Process For The Preparation Of Eszopiclone
摘要:本发明涉及一种制备6-(5-氯-2-吡啶基)-6,7-二氢-7-氧-5H-吡咯烷并[3,4-B]吡嗪-5-基-4-甲基哌嗪-1-羧酸酯,也称为唑吡克隆的方法.本发明进一步描述了一种有效的方法,用于将唑吡克隆分解为其对映体(eszopiclone和(R)-Zopiclone),并提供了一种(R)-Zopiclone的回收方法.制备(S)-6(S)-6-(5-氯-2-吡啶基)-6,7-二氢-7-氧-5H-吡咯烷并[3,4-B]吡嗪-5-基-4-甲基哌嗪-1-羧酸酯(eszopiclone)的方法包括以下步骤:在室温下将2-氨基5-氯吡啶与吡嗪-2,3-二羧酸酐反应,得到3-(5-氯吡啶-2-基)氨基甲酰基-2-吡嗪-2-羧酸;在第二惰性有机溶剂中环化3-(5-氯吡啶-2-基)氨基甲酰基-2-吡嗪-2-羧酸,得到6-(5-氯吡啶-2-基)5,7-二氧代-5,6-二氢吡咯烷并[3,4-B]-吡嗪;将6-(5-氯吡啶-2-基)5,7-二氧代-5,6-二氢吡咯烷并[3,4-B]-吡嗪还原,得到6-(5-氯吡啶-2-基)-5-羟基-7-氧-5,6-二氢吡咯烷并[3,4-B]吡嗪;在第三有机溶剂中,在三乙胺的存在下,加入催化量的酰化催化剂,与1-氯羰基-4-甲基哌嗪盐酸盐反应,得到混合型唑吡克隆;将唑吡克隆从烷基酯溶剂中结晶,然后在适当的醇或其混合物中纯化;通过用(+)-O-O'双苯甲酰酒石酸处理混合型唑吡克隆来分解唑吡克隆,从而得到eszopiclone.