Ortho C-H Hydroxyalkylation or Methylation of Aryl Iodides by Ethers and TMSI via a Catellani Strategy
Zhe Zhang1, Xi Chen1, Xue-Song Li1
1State Key Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou 730000, China.
Abstract:
In this paper, in the presence of trimethylsilyl iodide, the direct ortho-C-H hydroxyalkylation/methylation of aryl iodines was effectively realized via palladium/norbornene cooperative catalysis when low-cost tetrahydrofuran and 1,2-dimethoxyethane were used as alkyl sources. Heck, Suzuki, and Sonogashira coupling and hydrogenation were all compatible with the reaction as termination steps. In addition, neuromuscular agents and cardiovascular agents were synthesized in one step by this method, showing their potential application value.
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