A stereocontrolled construction of 2-azido-2-deoxy-1,2-cis-α- galactosidic linkages utilizing 2-azido-4,6-O-benzylidene-2- deoxygalactopyranosyl diphenyl phosphates: Stereoselective synthesis of mucin core 5 and core 7 structures

Kosuke Kakita, Toshifumi Tsuda, Noritoshi Suzuki, Seiichi Nakamura, Hisanori Nambu, Shunichi Hashimoto*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

13 Scopus citations

Abstract

TMSOTf-promoted glycosidation of 2-azido-4,6-O-benzylidene-2- deoxygalactosyl diphenyl phosphates with fluorenylmethoxycarbonyl (Fmoc)-protected serine and threonine derivatives in THF/Et 2O (1:1) gave glycosyl amino acids in high yields and with excellent levels of α-selectivity (α/β=94:6-95:5). The synthetic utility of the present glycosidation method was demonstrated by a stereoselective synthesis of mucin-type glycopeptide core 5 and core 7 building blocks, which are suitable for Fmoc-based solid-phase synthesis of O-glycopeptides.

Original languageEnglish
Pages (from-to)5005-5017
Number of pages13
JournalTetrahedron
Volume68
Issue number25
DOIs
StatePublished - 2012/06/24

Keywords

  • Carbohydrates
  • Glycosylation
  • Mucin
  • Phosphates
  • T -antigen

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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