Journal
ORGANIC LETTERS
Volume 23, Issue 15, Pages 6094-6098Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.1c02160
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Funding
- National Natural Science Foundation of China [22071214]
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An efficient method for the synthesis of [1,4]thiazino[4,3-alpha]indole derivatives was developed using sodium chlorodifluoroacetate and elemental sulfur as the difluoromethylthiolating reagent system. The sequential transformation process selectively formed four bonds including one C-N, two C-S, and one C-C bonds in good yields.
An efficient method for the synthesis of [1,4]thiazino[4,3-alpha]indole derivatives using sodium chlorodifluoroacetate (ClCF2CO2Na) and elemental sulfur as the difluoromethylthiolating reagent system has been developed. Three-component reactions of 2'-aminochalcones, sulfur, and ClCF2CO2Na under basic conditions using TEMPO as the oxidant afforded [1,4]thiazino[4,3-alpha]indol-10-ones containing a difluoromethyl thioether moiety in good yields. Four bonds including one C-N, two C-S, and one C-C bonds are selectively formed in the sequential transformation process.
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