Synthesis of the melatonin receptor agonist Ramelteon using a tandem C–H activation–alkylation/Heck reaction and subsequent asymmetric Michael addition |
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| Authors: | XiaoDan Fu XingQun Guo XingWei Li LiDong He YuShe Yang YouXi Chen |
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| Institution: | 1. Department of Medicinal Chemistry, Shanghai Sun-Sail Pharmaceutical Science & Technology Co., Ltd, No. 7, Building 1690, Cai-Lun Road, Zhangjiang Hi-Tech Park, Shanghai 201203, China;2. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, State Key Laboratory of Drug Research, 555 Zu-Chong-Zhi Road, Zhangjiang Hi-Tech Park, Shanghai 201203, China |
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| Abstract: | An asymmetric synthesis of the melatonin receptor agonist Ramelteon 1 has been achieved, which involved a tandem C–H activation–alkylation/Heck reaction and subsequent highly diastereoselective asymmetric Michael addition to generate the corresponding chiral intermediate, which was readily converted into Ramelteon 1 in 19% overall yield in 15 linear steps. |
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