Abstract
Well-defined ruthenium(II) phosphinous acid (PA) complexes enabled chemo-, site-, and diastereoselective C-H functionalization of arenes and alkenes with ample scope. The outstanding catalytic activity was reflected by catalyst loadings as low as 0.75 mol %, and the most step-economical access reported to date to angiotensin II receptor antagonist blockbuster drugs. Mechanistic studies indicated a kinetically relevant C-X cleavage by a single-electron transfer (SET)-type elementary process, and provided evidence for a PA-assisted C-H ruthenation step. A blockbuster catalyst: Well-defined ruthenium(II) phosphinous acid (PA) complexes were identified as powerful catalysts for highly selective C-H arylations with ample scope, which enabled low catalyst loadings and gave step-economical access to blockbuster drugs. Mechanistic studies were supportive of a PA-assisted C-H activation.
| Original language | English |
|---|---|
| Pages (from-to) | 1248-1252 |
| Number of pages | 5 |
| Journal | Chemistry - A European Journal |
| Volume | 22 |
| Issue number | 4 |
| DOIs | |
| State | Published - 22 Jan 2016 |
Bibliographical note
Publisher Copyright:© 2016 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.
Keywords
- C-H activation
- arylation
- kinetics
- reaction mechanisms
- ruthenium