Rh(iii)-catalyzed (5+2)-cycloaddition reactions of ortho-hydroxyethyl phenols with internal alkynes: efficient synthesis of benzoxepines

An unprecedented (5 + 2)-cycloaddition reaction of ortho-hydroxyethyl phenol and internal alkyne was developed. This Rh(iii)-catalyzed reaction provided benzoxepine derivatives which have very high biological significance. A wide range of ortho-hydroxyethyl phenols and internal alkynes were studied to provide the benzoxepines in high yields.

Automated summary

An unprecedented (5 + 2)-cycloaddition reaction between ortho-hydroxyethyl phenol and internal alkyne was developed using rhodium(iii) catalysis. This reaction provided benzoxepine derivatives with high biological significance. A wide range of ortho-hydroxyethyl phenols and internal alkynes were effectively used to obtain high yields of benzoxepines.