Improved method for synthesizing dolutegravir

The invention relates to an improved method for synthesizing dolutegravir and belongs to the field of medicinal chemistry. The method takes maltol (compound 1) as a raw material, and a target is synthesized by the following route. The process raw material is cheap and easy to obtain, a reaction solv...

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Hauptverfasser: ZHANG FANGJIE, CHEN SHUIKU, ZHU SONGLIN, ZHU HUIFENG, CUI HAO, LI XUGUANG, LIU CONGJUN, LUO QI, MENG QINGLE, FANG SHUIXIA
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention relates to an improved method for synthesizing dolutegravir and belongs to the field of medicinal chemistry. The method takes maltol (compound 1) as a raw material, and a target is synthesized by the following route. The process raw material is cheap and easy to obtain, a reaction solvent can be recycled, the post-treatment operation is simple, the yield and the purity are high, especially the carbamoylation and debenzylation reaction are carried out in one step, the synthesis route is simplified, the cost is reduced, and the large-scale industrial production is facilitated. 本发明涉及种改进的度鲁特韦的合成方法,属药物化学领域。该方法以麦芽酚(化合物1)为原料,采用如下路线合成目标物。该工艺原料廉价易得,反应溶剂可回收再利用,后处理操作简便,收率及纯度高,尤其是胺甲酰化和脱苄基反应步进行,简化了合成路线,节约了成本,利于规模化工业生产。。