Carboxylate-Directed Pd-Catalyzed β-C(sp<SUP>3</SUP>)-H Arylation of <i>N</i>-Methyl Alanine Derivatives for Diversification of Bioactive Peptides

  • Yeom, Suyeon; 
  • Kim, Do Young; 
  • Kim, Seungwoo; 
  • Gontala, Arjun; 
  • Park, Jimin; 
  • ... Kim, Hak Joong; 
  • 외 1명
Citations

WEB OF SCIENCE

4
Citations

SCOPUS

4

초록

This study presents a Pd(II)-catalyzed method for the beta-C(sp(3))-H arylation of N-Cbz- or N-Fmoc-protected N-methyl alanines, providing ready access to building blocks for N-methylated peptide synthesis. For this transformation, the native carboxylate was exploited as the directing group, attributing its success to the use of a monoprotected amino-pyridine ligand. Its synthetic utility was demonstrated by facile generation of nine analogues of the naturally occurring N-methylated cyclic peptide cycloaspeptide A.

키워드

C-H FUNCTIONALIZATION; AMINO-ACIDS; C(SP(3))-H ARYLATION; BOND FUNCTIONALIZATION; CYCLIC PENTAPEPTIDES; COUPLING REACTIONS; LIGAND
제목
Carboxylate-Directed Pd-Catalyzed β-C(sp<SUP>3</SUP>)-H Arylation of <i>N</i>-Methyl Alanine Derivatives for Diversification of Bioactive Peptides
저자
Yeom, Suyeon; Kim, Do Young; Kim, Seungwoo; Gontala, Arjun; Park, Jimin; Lee, Yong Ho; Kim, Hak Joong
DOI
10.1021/acs.orglett.3c03616
발행일
2023-12-12
유형
Article
저널명
Organic Letters
권
25
호
50
페이지
9008 ~ 9013