Journal
ORGANIC LETTERS
Volume 22, Issue 17, Pages 6932-6937Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.0c02487
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Funding
- National Science Foundation of China [21472151]
- Natural Science Foundation of Chongqing [cstc2019jcyj-msxmX0414]
- Fundamental Research Funds for the Central Universities [XDJK2019AA003]
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An efficient enantioselective synthesis of cyclic alpha-aminophosphonates via multicomponent reactions of 2-alkynylbenzaldehydes, amines, and dimethylphosphonate has been developed with the use of a chiral silver spirocyclic phosphate as the catalyst. This protocol provides straightforward access to a series of chiral C1-phosphonylated 1,2-dihydroisoquinoline derivatives with high yields (up to 99%) and high enantioselectivities (up to 94% ee) for a broad substrate scope. The products could be further transformed into densely functionalized compounds and corresponding alpha-aminophosphonic acids.
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