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Enantioselective Alkynylation of Isatins: A Combination of Metal Catalysis and Organocatalysis.

Dan JiangPei TangQiuyuan TanZhao YangLing HeMin Zhang
Published in: Chemistry (Weinheim an der Bergstrasse, Germany) (2020)
An efficient and catalytic asymmetric alkynylation of isatins has been developed using a bifunctional amidophosphine-urea/AgBF4 complex as the catalyst. By a combination of metal catalysis and organocatalysis, excellent enantioselectivities (up to 99 % ee) and good yields are achieved. A wide range of both terminal alkynes and isatins are tolerated by this new catalyst system, providing access to structurally diverse propargylic alcohols with tetrasubstituted stereogenic centers in high efficiency.
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