Journal
CHEMICAL COMMUNICATIONS
Volume 53, Issue 14, Pages 2222-2225Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c6cc09643c
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Funding
- Recruitment Program of Global Experts (1000 Talents Plan)
- Natural Science Foundation of Fujian Province [2016J01064]
- Fujian Hundred Talents Plan and Program of Innovative Research Team of Huaqiao University [Z14X0047]
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An original and efficient synthesis of 3,3-difluoro-2-oxindole derivatives has been developed via copper/B(2)pin(2)-catalyzed difluoroacetylation of aniline via C-H activation followed by intramolecular amidation. In this method, amino groups in primary, secondary or tertiary anilines act as directing groups, providing ortho-difluoroacetylated products regio-selectively. And in the first two cases, further intramolecular amidation affords 3,3-difluoro-2-oxindole derivatives via a one-pot strategy. This method facilitates the synthesis of compound A as a potent and selective EP3 receptor antagonist in only five steps in 13% yield instead of the previously reported nine steps in overall 4% yield.
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