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1. WO2015128687 - CONTINUOUS FLOW PEPTIDE SYNTHESIS

Publication Number WO/2015/128687
Publication Date 03.09.2015
International Application No. PCT/HU2015/000022
International Filing Date 27.02.2015
IPC
C07K 1/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General processes for the preparation of peptides
04on carriers
CPC
C07K 1/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General methods for the preparation of peptides ; , i.e. processes for the organic chemical preparation of peptides or proteins of any length
C07K 1/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General methods for the preparation of peptides ; , i.e. processes for the organic chemical preparation of peptides or proteins of any length
04on carriers
C07K 1/042
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General methods for the preparation of peptides ; , i.e. processes for the organic chemical preparation of peptides or proteins of any length
04on carriers
042characterised by the nature of the carrier
C07K 1/045
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General methods for the preparation of peptides ; , i.e. processes for the organic chemical preparation of peptides or proteins of any length
04on carriers
045using devices to improve synthesis, e.g. reactors, special vessels
C07K 1/061
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General methods for the preparation of peptides ; , i.e. processes for the organic chemical preparation of peptides or proteins of any length
06using protecting groups or activating agents
061using protecting groups
C07K 1/10
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General methods for the preparation of peptides ; , i.e. processes for the organic chemical preparation of peptides or proteins of any length
10using coupling agents
Applicants
  • SZEGEDI TUDOMÁNYEGYETEM [HU]/[HU]
Inventors
  • FÜLÖP, Ferenc
  • MÁNDITY, István
  • OLASZ, Balázs
Agents
  • SBGK PATENT AND LAW OFFICES
Priority Data
HU P140011428.02.2014HU
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) CONTINUOUS FLOW PEPTIDE SYNTHESIS
(FR) SYNTHÈSE DE PEPTIDES EN FLUX CONTINU
Abstract
(EN) The invention is directed to a continuous flow chemical method for the solid phase synthesis of peptides at elevated temperatures and pressures. The invention is based on the unexpected finding that using the continuous flow technology to the solid phase peptide synthesis the amino acid excess can be reduced to a range of 1 to 1.5 equivalents and peptides of high purity can be synthesized with practically complete couplings and in good yields if the synthesis is performed at elevated temperature and pressure. According to the invention nearly 100% coupling can be reached also when using low amino acid excess during the peptide synthesis and even in the case of peptides comprising strongly structure promoting amino acids the yields are excellent.
(FR) Cette invention concerne un procédé chimique en flux continu pour la synthèse en phase solide de peptides à des températures et des pressions élevées. L'invention se base sur l'inattendue découverte selon laquelle l'application de la technologie en flux continu à la synthèse des peptides en phase solide permet de réduire l'acide aminé en excédent à une fourchette de 1 à 1,5 équivalent et de synthétiser des peptides de haute pureté à des couplages pratiquement complets et de bons rendements si la synthèse est réalisée à une température et à une pression élevées. Selon l'invention, un couplage de pratiquement 100 % peut être atteint même en utilisant un faible excédent d'acide aminé pendant la synthèse des peptides et même dans le cas de peptides comprenant des acides aminés favorisant fortement la structure, les rendements sont excellents.
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