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1. EP0075017 - NEW PROCESS FOR SYNTHESIZING A POLYPEPTIDE.

Office
European Patent Office
Application Number 82901513
Application Date 11.03.1982
Publication Number 0075017
Publication Date 30.03.1983
Publication Kind A1
IPC
C07D 263/44
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
263Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
02not condensed with other rings
30having two or three double bonds between ring members or between ring members and non-ring members
34with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
44Two oxygen atoms
C07C 103/52
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
103Carboxylic acid amides
30N-substituted carboxylic acid amides
32of acyclic saturated carboxylic acids
50Amides of acyclic saturated amino carboxylic acids
52Peptides
C07K 1/02
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General processes for the preparation of peptides
02in solution
C07D 263/44
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
263Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
02not condensed with other rings
30having two or three double bonds between ring members or between ring members and non-ring members
34with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
44Two oxygen atoms
C07K 1/113
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General processes for the preparation of peptides
107by chemical modification of precursor peptides
113without change of the primary structure
C07K 5/075
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
06Dipeptides
072the side chain of the first amino acid containing more carboxyl groups than amino groups, or derivatives thereof, e.g. Asp, Glu, Asn
075Asp-Phe; Derivatives thereof, e.g. aspartame
CPC
C07D 263/44
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
263Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
02not condensed with other rings
30having two or three double bonds between ring members or between ring members and non-ring members
34with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
44Two oxygen atoms
C07K 5/0613
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
06Dipeptides
06104with the first amino acid being acidic
06113Asp- or Asn-amino acid
06121the second amino acid being aromatic or cycloaliphatic
0613Aspartame
Applicants FLORK MICHEL
GRINDA JEAN ROBERT
Inventors FLORK MICHEL
Designated States
Priority Data 8104817 11.03.1981 FR
Title
(DE) NEUES VERFAHREN ZUR SYNTHETISIERUNG EINES POLYPEPTIDES.
(EN) NEW PROCESS FOR SYNTHESIZING A POLYPEPTIDE.
(FR) NOUVEAU PROCEDE DE SYNTHESE D'UN POLYPEPTIDE.
Abstract
(EN) New process for the synthesis of methyl L-$g(a)-aspartyl phenyl alaninate comprising the esterification of phenylalaninate by methanol into methyl ester, the condensation of the latter with a mixed carbonic-L-aspartic anhydride in alkaline medium and the decarboxylation of the methyl N-carboxy L-$g(a)-aspartyl phenyl alaninate formed in an acid medium. The product thus obtained may be used as a sweetener in the pharmaceutical or food industry.
(FR) Nouveau procédé de synthèse du L-$g(a)-aspartyl phenyl alaninate de méthyle qui consiste à estérifier la phénylalaninate par le méthanol en ester méthylique, à condenser celui-ci avec un anhydride mixte carbonique - L - aspartique en milieu alcalin et à décarboxyler le N - carboxy L -$g(a)-aspartyl phényl alaninate de méthyle formé en milieu acide. Le produit ainsi obtenu trouve un emploi comme édulcorant dans l'industrie pharmaceutique ou alimentaire.
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