Ligand for C-H Borylation of Substituted Benzenes

　Segawa, Itami et al. reported that a complex formed from 2,2'-bis[bis(3,5-dimethylphenyl)phosphino]-1,1'-biphenyl (1) and an iridium complex catalyzed regioselective borylation.¹⁾ This C-H borylation proceeds on 1,2-disubstituted benzene with high para-selectivity from the larger substituent. In addition, this reaction has a high tolerance to various kinds of functional groups, so that it is applicable to the synthesis at the final of synthesis and further conversion from the installed boryl group is possible. Thus, its use is anticipated in medicinal chemistry. The iridium complex can also catalyze the para-selective C-H borylation of mono-substituted benzenes with good regioselectivity.²⁾

References

• 1) Selective Transformation of Strychnine and 1,2-Disubstituted Benzenes by C-H Borylation
  • Y. Saito, K. Yamanoue, Y. Segawa, K. Itami, Chem 2020, 6, 985.
• 2) para-C-H Borylation of Benzene Derivatives by a Bulky Iridium
  • Y. Saito, Y. Segawa, K. Itami, J. Am. Chem. Soc. 2015, 137, 5139.

Related Compounds

B1964

Bis(pinacolato)diboron (B₂(pin)₂)

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