In situ neutralization in Boc‐chemistry solid phase peptide synthesis: Rapid, high yield assembly of difficult sequences

  • SCHNölzer, MARTINA
  • ALEWOOD, PAUL
  • JONES, ALUN
  • ALEWOOD, DIANNE
  • KENT, STEPHEN B.H.
Publication date
January 1992
Publisher
Wiley
ISSN
0367-8377
Citation count (estimate)
826

Abstract

Simple, effective protocols have been developed for manual and machine‐assisted Boc‐chemistry solid phase peptide synthesis on polystyrene resins. These use in situ neutralization [i.e. neutralization simultaneous with coupling], high concentrations (> 0.2 M) of Boc‐amino acid‐OBt esters plus base for rapid coupling, 100% TFA for rapid Boc group removal, and a single short (30 s) DMF flow wash between deprotection/coupling and between coupling/deprotection. Single 10 min coupling times were used throughout. Overall cycle times were 15 min for manual and 19 min for machine‐assisted synthesis (75 residues per day). No racemization was detected in the base‐catalyzed coupling step. Several side reactions were studied, and eliminated. These incl...

Extracted data

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