Journal
ADVANCED SYNTHESIS & CATALYSIS
Volume 361, Issue 6, Pages 1441-1446Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/adsc.201801378
Keywords
C-H activation; Palladium; Transient directing group; Indoles; Regioselective
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Funding
- DST, India [SR/NM/NS-1065/2015 (G)]
- SERB [EMR/2015/002047]
- DST-Fast Track Young Scientist, CSIR
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A convergent strategy for the synthesis of biologically relevant C4-substituted indole scaffolds was demonstrated using Pd(II)-catalyzed remote C-H functionalization of indoles and azaindoles. The reaction displays high regioselectivity for the C4-position of indole-3-carbaldehydes using glycine as an inexpensive transient directing group. Notable features of this transformation include the selective formation of six-membered palladacyle and excellent functional group tolerance.
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