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Convenient One‐Pot Room Temperature Synthesis of 2‐(trifluoromethyl)‐1,2,3,4,7,8‐hexahydroquinolin‐5(6H)‐one derivatives via Catalyst‐Free Multicomponent Reactions
Authors:Rong Liang‐Ce  Shimin Tao  Yunyun Zha  Sheng Xia  Yanian Gao  Ming Chen
Affiliation:College of Chemistry and Chemical Engineering, Key Laboratory of Biotechnology for Medicinal Plant, Jiangsu Normal University, Xuzhou, Jiangsu, People's Republic of China
Abstract:This paper describes an efficient approach for the synthesis of 2‐(trifluoromethyl)‐1,2,3,4,7,8‐hexahydroquinolin‐5(6H)‐one derivatives via a one‐pot four‐component reaction of aromatic aldehyde, 5,5‐dimethylcyclohexane‐1,3‐dione, 4,4,4‐trifluoro‐1‐(thien‐2‐yl)butane‐1,3‐dione, and NH4OAc with excellent yields at room temperature. In this synthesis, the trifluoromethyl was efficiently introduced in hexahydroquinoline structure, and they may be valuable the drug candidates. This approach also offered several other advantages, such as catalyst‐free, mild conditions, and simple experimental operation.
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