Title:
PEPTIDE SYNTHESIS METHOD
Document Type and Number:
WIPO Patent Application WO/2016/140232
Kind Code:
A1
Abstract:
The present invention pertains to a peptide synthesis reaction using a carrier which can reversibly repeat a dissolved state and an encapsulated state, wherein it is easy to solve the problem of amino acid active species which are present in a reaction system during a deprotection reaction. The present invention (1) provides a peptide synthesis method containing the following steps: a step in which an N-Fmoc protected amino acid and a peptide having a C-terminus protected by a carrier is crystallized together with changes in the composition of a solvent in which the peptide is dissolved are condensated, in the presence of a condensing agent, to obtain an N-Fmoc-C-carrier protected peptide; a step in which a C1-14 alkyl amine or hydroxylamine is added to the reaction system; a step in which the N terminal is deprotected; and a separation step in which a solvent composition having a C-carrier protected peptide dissolved therein is varied, thereby crystallizing said peptide.
Inventors:
KONO YUSUKE (JP)
SUZUKI HIDEAKI (JP)
MUTO SUSUMU (JP)
SUZUKI HIDEAKI (JP)
MUTO SUSUMU (JP)
Application Number:
PCT/JP2016/056319
Publication Date:
September 09, 2016
Filing Date:
March 02, 2016
Export Citation:
Assignee:
JITSUBO CO LTD (JP)
International Classes:
C07C43/225; C07K1/10; C07C43/23; C07C217/58
Domestic Patent References:
| WO2007034812A1 | 2007-03-29 | |||
| WO2007122847A1 | 2007-11-01 | |||
| WO2007099656A1 | 2007-09-07 |
Foreign References:
| JP2003183298A | 2003-07-03 | |||
| JP2004059509A | 2004-02-26 | |||
| JPH06509821A | 1994-11-02 | |||
| JP2003500415A | 2003-01-07 |
Other References:
CARPINO, L.A. ET AL.: "Rapid, Continuous Solution-Phase PeptideSynthesis: Application to Peptides of Pharmaceutical Interest", ORG. PROCESS RES. DEV., vol. 7, no. 1, 2003, pages 28 - 37, XP055008431, ISSN: 1083-6160, DOI: doi:10.1021/op0202179
EGGEN, I.F. ET AL.: "A novel method for repetitive peptide synthesis in solution without isolation of intermediates", J. PEPT. SCI., vol. 11, no. 10, 2005, pages 633 - 641, XP002420466, ISSN: 1099-1387, DOI: doi:10.1002/psc.670
See also references of EP 3266792A4
EGGEN, I.F. ET AL.: "A novel method for repetitive peptide synthesis in solution without isolation of intermediates", J. PEPT. SCI., vol. 11, no. 10, 2005, pages 633 - 641, XP002420466, ISSN: 1099-1387, DOI: doi:10.1002/psc.670
See also references of EP 3266792A4
Attorney, Agent or Firm:
OSAWA, KENICHI (JP)
Ken-ichi Osawa (JP)
Ken-ichi Osawa (JP)
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