Rh(III)-catalyzed regioselective versatile indole derivatization: delivering potential of rare β-(1 H-indol-2-yl)-β-amino acids in one pot

Shuaizhong Zhang; Jinquan Zhang; Hongbin Zou

doi:10.1039/d3cc01289a

Rh(III)-catalyzed regioselective versatile indole derivatization: delivering potential of rare β-(1 H-indol-2-yl)-β-amino acids in one pot

Chem Commun (Camb). 2023 Apr 20;59(33):4978-4981. doi: 10.1039/d3cc01289a.

Authors

Shuaizhong Zhang¹, Jinquan Zhang¹, Hongbin Zou¹

Affiliation

¹ College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang, 310058, P. R. China. zouhb@zju.edu.cn.

PMID: 37017210
DOI: 10.1039/d3cc01289a

Abstract

Rh-catalyzed selective C-H functionalization of indoles with two routes was developed: an alkenylation-annulation with the addition of KHSO₄ and alkenylation-elimination in the presence of CsOAc to the corresponding products, respectively. Notably, one-pot hydrolysis and benzoylation of the annulation products successfully afforded easily separable β-(1H-indol-2-yl)-β-amino acid derivatives.