Organocatalytic asymmetric domino aza-Michael-Mannich reaction: synthesis of tetrahydroimidazopyrimidine derivatives |
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| Authors: | Li Hong Zhao Junling Zeng Lili Hu Wenhui |
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| Institution: | Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou Science Park, Guangdong 510530, People's Republic of China. |
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| Abstract: | Highly substituted tetrahydroimidazopyrimidine derivatives with three chiral centers have been synthesized for the first time using an organocatalytic asymmetric domino aza-Michael-Mannich reaction of α,β-unsaturated aldehydes and N-arylidene-1H-imidazol-2-amines. This efficient approach furnishes the products in good yields (42-87%) with excellent stereoselectivities (>20:1 dr, up to >99% ee). |
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