Journal
ORGANIC LETTERS
Volume 22, Issue 13, Pages 5014-5019Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.0c01578
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Funding
- National Natural Science Foundation of China [81972824, 21861009]
- Guangdong Provincial Key Laboratory of Chiral Molecule and Drug Discovery [2019B030301005]
- Science and Technology Program of Guangzhou [201607010118]
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A catalytic asymmetric umpolung cross-Mannich reaction of cyclic ketimines is realized. This protocol provides an efficient methodology for the facile synthesis of chiral vicinal tetrasubstituted diamines in high yields with excellent chemo-, regio-, diastereo-, and enantioselectivities using cinchona-derived bifunctional organocatalysts (85-98% yield, up to >20:1 dr, and >99% ee).
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