An efficient approach for the direct synthesis of alkylated 4-hydroxycoumarin derivatives via a Cu-catalyzed cascade dehydrogenation/conjugate addition sequence starting from simple saturated ketones and 4-hydroxycoumarins has been developed. This protocol features excellent functional-group tolerance, easy scale-up, and a broad substrate scope including bioactive molecules. More importantly, a series of marketed drugs, such as warfarin, acenocoumarol, coumachlor, and coumafuryl, can be obtained by this method.
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Dalian Polytech Univ, Sch Light Ind & Chem Engn, Dalian 116034, Peoples R China
Chinese Acad Sci, Dalian Inst Chem Phys, Dalian 116023, Peoples R ChinaDalian Polytech Univ, Sch Light Ind & Chem Engn, Dalian 116034, Peoples R China
Guo, Wei-Lei
Hou, Chuan-Jin
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Dalian Polytech Univ, Sch Light Ind & Chem Engn, Dalian 116034, Peoples R ChinaDalian Polytech Univ, Sch Light Ind & Chem Engn, Dalian 116034, Peoples R China
Hou, Chuan-Jin
Duan, Zheng-Chao
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Chinese Acad Sci, Dalian Inst Chem Phys, Dalian 116023, Peoples R ChinaDalian Polytech Univ, Sch Light Ind & Chem Engn, Dalian 116034, Peoples R China
Duan, Zheng-Chao
Hu, Xiang-Ping
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Chinese Acad Sci, Dalian Inst Chem Phys, Dalian 116023, Peoples R ChinaDalian Polytech Univ, Sch Light Ind & Chem Engn, Dalian 116034, Peoples R China