Journal
SYNLETT
Volume 26, Issue 4, Pages 531-536Publisher
GEORG THIEME VERLAG KG
DOI: 10.1055/s-0034-1379606
Keywords
C-H arylation; benzothiophene; benzofuran; MIDA boronate; bis(alkoxo)palladium(II) complex
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Funding
- National Science Foundation of China [21172200]
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With high regioselectivity, a series of benzoheterocyclic compounds were synthesized via palladiium-catalyzed phosphine-free C-H arylation of benzothiophenes/benzofurans with aryl MIDA boronates at 30-50 degrees C in moderate to excellent yields. MIDA boronates were used in C-H arylation of heterocycles for the first time. Under the optimal conditions, the benzothiophenes could be transformed into the beta-arylbenzothiophenes, and the benzofurans gave only alpha-aryl-substituted products.
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