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Pd‐Catalyzed Late‐Stage Monoacetoxylation and Monoiodination of 4‐Alkyl‐1,5‐diaryl‐1 H‐pyrazole‐3‐carboxylates via Direct Csp2−H Bond Activation

Pd‐Catalyzed Late‐Stage Monoacetoxylation and Monoiodination of 4‐Alkyl‐1,5‐diaryl‐1... A palladium‐catalyzed, late‐stage functionalization of 4‐alkyl‐1,5‐diaryl‐1 H‐pyrazole‐3‐carboxylates to achieve acetoxylation or iodination via Csp2−H bond activation with synthetically useful to excellent yields is described. These straightforward transformations feature highly functionalized substrates, excellent site selectivity, rapid reaction, and simple operation. The C−O and C−I bond‐forming protocols allow convenient accesses to lots of complex monoacetoxylated and monoiodinated products from pharmaceutically important intermediates. Iodoacetic acid is also used as the iodinating agent in C−H bond activation. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Asian Journal of Organic Chemistry Wiley

Pd‐Catalyzed Late‐Stage Monoacetoxylation and Monoiodination of 4‐Alkyl‐1,5‐diaryl‐1 H‐pyrazole‐3‐carboxylates via Direct Csp2−H Bond Activation

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References (92)

Publisher
Wiley
Copyright
© 2016 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinheim
ISSN
2193-5807
eISSN
2193-5815
DOI
10.1002/ajoc.201600028
Publisher site
See Article on Publisher Site

Abstract

A palladium‐catalyzed, late‐stage functionalization of 4‐alkyl‐1,5‐diaryl‐1 H‐pyrazole‐3‐carboxylates to achieve acetoxylation or iodination via Csp2−H bond activation with synthetically useful to excellent yields is described. These straightforward transformations feature highly functionalized substrates, excellent site selectivity, rapid reaction, and simple operation. The C−O and C−I bond‐forming protocols allow convenient accesses to lots of complex monoacetoxylated and monoiodinated products from pharmaceutically important intermediates. Iodoacetic acid is also used as the iodinating agent in C−H bond activation.

Journal

Asian Journal of Organic ChemistryWiley

Published: Apr 1, 2016

Keywords: ; ; ; ;

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