- Metal-Free C–S Bond Cleavage to Access N-Substituted Acrylamide and β-Aminopropanamide
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Metal-free and Selectfluor-mediated C–S bond cleavage is described. This novel strategy provides a facile and efficient method to access important N-substituted acrylamide and β-aminopropanamide derivatives with good functional group tolerance and yields.
- Yang, Ke,Li, Yi,Ma, Zhiyan,Tang, Long,Yin, Yue,Zhang, Hao,Li, Zhengyi,Sun, Xiaoqiang
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- LiCl-promoted amination of β-methoxy amides (γ-lactones)
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An efficient and mild method has been developed for the amination of β-methoxy amides (γ-lactones) including natural products michelolide, costunolide and parthenolide derivatives by using lithium chloride in good yields. This reaction is applicable to a wide range of substrates with good functional group tolerance. Mechanism studies show that the reactions undergo a LiCl promoted MeOH elimination from the substrates to form the corresponding α,β-unsaturated intermediates followed by the Michael addition of amines.
- Jia, Wen-Qiang,Pan, Xian-Dao,Shen, Long-Ying,Wang, Xiao-Jian,Zeng, Bing-Lin,Zhao, Hong-Yi,Zhao, Ru
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p. 34938 - 34942
(2020/10/14)
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- Consequences of linker length alteration of the α7 nicotinic acetylcholine receptor (nAChR) agonist, SEN12333
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A series of ligands based on SEN12333, containing either contracted or elongated alkyl chains, were synthesized and evaluated in molecular docking studies against a homology model of the α7 nicotinic acetylcholine receptor (nAChR) subtype. The predicted binding of all ligands was highly similar, with the exception of the analog containing a 5 methylene unit spacer. However, in vitro competition binding assays revealed that the ligands possessed dissimilar binding affinities, with a Ki range of more than an order of magnitude (Ki = 0.50 to >10 μM), and only SEN12333 itself exhibited functional activity at the α7 nAChR.
- Beinat, Corinne,Banister, Samuel D.,Van Prehn, Saundra,Doddareddy, Munikumar Reddy,Hibbs, David,Sako, Michael,Chebib, Mary,Tran, Thao,Al-Muhtasib, Nour,Xiao, Yingxian,Kassiou, Michael
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supporting information; experimental part
p. 2380 - 2384
(2012/05/05)
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