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Enantioselective Copper-Catalyzed Remote C(sp3)-H Alkynylation of Linear Primary Sulfonamides.
Organic Letters ( IF 6.091 ) Pub Date : 2020-05-05 , DOI: 10.1021/acs.orglett.0c01325
Cheng-Yu Wang,Zi-Yang Qin,Yu-Ling Huang,Yi-Ming Hou,Ruo-Xing Jin,Chao Li,Xi-Sheng Wang

The highly efficient copper-catalyzed enantioselective alkynylation of the remote C(sp3)-H bond on linear primary sulfonamides is presented here using a radical relay strategy. The chiral box-copper complex, which is used to recapture the in-situ-generated alkyl radical via a 1,5-HAT strategy, is the key to success, affording the chiral alkynes after a following reductive elimination. A general substrate scope, mild conditions, and excellent regio- and enantioselective control are demonstrated in this method.
更新日期:2020-05-05

 

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