期刊
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
卷 2015, 期 34, 页码 7433-7437出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ejoc.201501048
关键词
Amides; Fused-ring systems; Drug design; Oxidation; Ozonolysis
资金
- Council of Scientific and Industrial Research (CSIR), New Delhi through the NICE-P program (XII Five Year Plan) [CSC0109]
- University Grants Commission (UGC)
- CSIR, New Delhi
A simple and convenient method to access 4-quinolone-3-carboxylic acid amides from indole-3-acetic acid amides through one-pot oxidative cleavage of the indole ring followed by condensation (Witkop-Winterfeldt type oxidation) was explored. The scope of the method was confirmed with more than 20 examples and was successfully applied to the synthesis of the drug Ivacaftor, the most expensive drug on the market.
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