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Diastereo- and Enantioselective Mannich/Cyclization Cascade Reaction Access to Chiral Benzothiazolopyrimidine Derivatives |
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| Authors: | Yan Zhang Jia-Hui Yang Ying-Qi Xia Lin Dong Fen-Er Chen |
| Affiliation: | 1. Sichuan Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University, Chengdu, 610041 P. R. China These authors contributed equally to this work.;2. Sichuan Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University, Chengdu, 610041 P. R. China |
| Abstract: | An efficient asymmetric Mannich/cyclization cascade strategy was established from 2-benzothiazolimines with N-acylpyrazoles to provide optical active benzothiazolopyrimidine derivatives using a copper-based complex. The mild cascade process constructed various structurally diverse products with broad scope of substrates together with excellent enantioselectivities (up to 99 % ee) and diastereoselectivities (up to 99:1 d.r.). |
| Keywords: | 2-benzothiazolimines asymmetric catalysis chiral benzothiazolopyrimidine Mannich/cyclization cascade reaction N-acylpyrazoles |