N-叔丁基亚磺酰基-3,3,3-三氟乙醛亚胺的不对称傅克反应：对映体纯的含1-氨基-2,2,2-三氟乙基吲哚的通用合成方法
Asymmetric Friedel-Crafts reactions of N-tert-butylsulfinyl-3,3,3-trifluoroacetaldimines: general access to enantiomerically pure indoles containing a 1-amino-2,2,2-trifluoroethyl group.
作者信息
Wu Lingmin, Xie Chen, Mei Haibo, Soloshonok Vadim A, Han Jianlin, Pan Yi
机构信息
School of Chemistry and Chemical Engineering, Nanjing University , Nanjing 210093, China.
出版信息
J Org Chem. 2014 Aug 15;79(16):7677-81. doi: 10.1021/jo5012009. Epub 2014 Jul 28.
PMID:25051149
Abstract
We have demonstrated that 3,3,3-trifluoroacetaldimine (S)-1 easily reacts with indole derivatives under Friedel-Crafts reactions to provide reliable and generalized access to biologically interesting compounds containing the CF3CH(NH2)- pharmacophoric group. The reactions proceed with high rates and generally excellent yields (>90%) and stereochemical outcomes (99:1 dr).
摘要
我们已经证明，3,3,3-三氟乙醛亚胺（S）-1在傅克反应条件下能与吲哚衍生物轻松反应，从而可靠且广泛地获得含有CF3CH(NH2)-药效基团的具有生物学意义的化合物。这些反应速率高，产率通常优异（>90%），立体化学结果也很好（非对映体比例为99:1）。
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