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Title: Feedstocks to Pharmacophores: Cu-Catalyzed Oxidative Arylation of Inexpensive Alkylarenes Enabling Direct Access to Diarylalkanes

A Cu-catalyzed method has been identified for selective oxidative arylation of benzylic C–H bonds with arylboronic esters. The resulting 1,1-diarylalkanes are accessed directly from inexpensive alkylarenes containing primary and secondary benzylic C–H bonds, such as toluene or ethylbenzene. All catalyst components are commercially available at low cost, and the arylboronic esters are either commercially available or easily accessible from the commercially available boronic acids. In conclusion, the potential utility of these methods in medicinal chemistry applications is highlighted.
Authors:
 [1] ;  [2] ; ORCiD logo [1]
  1. Univ. of Wisconsin-Madison, Madison, WI (United States)
  2. Univ. of Wisconsin-Madison, Madison, WI (United States); Merck & Co., Inc., Rahway, NJ (United States)
Publication Date:
Grant/Contract Number:
FG02-05ER15690
Type:
Accepted Manuscript
Journal Name:
Journal of the American Chemical Society
Additional Journal Information:
Journal Volume: 139; Journal Issue: 23; Journal ID: ISSN 0002-7863
Publisher:
American Chemical Society (ACS)
Research Org:
Univ. of Wisconsin-Madison, Madison, WI (United States)
Sponsoring Org:
USDOE Office of Science (SC), Basic Energy Sciences (BES) (SC-22)
Country of Publication:
United States
Language:
English
Subject:
37 INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY
OSTI Identifier:
1471697