Abstract

The present invention relates to a process for extraction of a peptide from a reaction mixture resulting from a peptide coupling reaction, the reaction mixture containing the peptide and a polar aprotic solvent selected from the group consisting of N,N- dimethylformamide, A/,A/-dimethylacetamide and A/-methyl-2-pyrrolidone, whereby the process comprises a step a) and a step b): step a) comprises the addition of a component a1) and a component a2), whereby component a1) is 2-methyltetrahydrofuran and component a2) is water, to the reaction mixture, so that a biphasic system with an organic layer and an aqueous layer is obtained; step b) comprises the subsequent separation of the organic layer containing the peptide from the aqueous layer. In a particularly preferred embodiment of the present invention, a combination of 2- methyltetrahydrofuran and an organic solvent 1 selected from the group consisting of n-heptane, toluene, ethylacetate, isopropylacetate, acetonitrile and tetrahydrofuran is used for the process for extraction. The extraction step is preferably used in a process for preparation of a peptide in liquid phase.

IPC Classes  ?

• C07K 1/02 - General processes for the preparation of peptides in solution
• C07K 1/14 - Extraction; Separation; Purification

Abstract

The present invention relates to a process for extraction of a peptide from a reaction mixture resulting from a peptide coupling reaction, the reaction mixture containing the peptide and a polar aprotic solvent selected from the group consisting of N,N- dimethylformamide, N,N-dimethylacetamide and N-methyl-2-pyrrolidone, whereby the process comprises a step a) and a step b): step a) comprises the addition of a component a1) and a component a2), whereby component a1 ) is toluene and component a2) is water, to the reaction mixture, so that a biphasic system with an organic layer and an aqueous layer is obtained; step b) comprises the subsequent separation of the organic layer containing the peptide from the aqueous layer. In a particularly preferred embodiment of the present invention, a combination of toluene and an organic solvent 1 selected from the group consisting of n-heptane, 2- methyltetrahydrofuran, ethylacetate, isopropylacetate, acetonitrile and tetrahydrofuran is used for the process for extraction. The extraction step is preferably used in a process for preparation of a peptide in liquid phase.

IPC Classes  ?

• C07K 1/14 - Extraction; Separation; Purification

Abstract

The present invention relates to a process for extraction of a peptide from a reaction mixture resulting from a peptide coupling reaction, the reaction mixture containing the peptide and a polar aprotic solvent selected from the group consisting of Λ/,Λ/-dimethylformamide, A/,A/-dimethylacetamide and A/-methyl-2-pyrrolidone, whereby the process comprises a step a) and a step b):step a) comprises the addition of a component a1 ), a component a2) and a component a3), whereby component a1) is an organic solvent 1, the organic solvent 1 is selected from the group consisting of 2-methyltetrahydrofuran and toluene, component a2) is water, and component a3) is an organic solvent 2, the organic solvent 2 is selected from the group consisting of ethylacetate, isopropylacetate, acetonitrile, tetrahydrofuran and n-heptane to the reaction mixture, so that a biphasic system with an organic layer and an aqueous layer is obtained; step b) comprises the subsequent separation of the organic layer containing the peptide from the aqueous layer. The extraction step is preferably used in a process for preparation of a peptide in liquid phase.

IPC Classes  ?

• C07K 1/14 - Extraction; Separation; Purification
• C07K 1/02 - General processes for the preparation of peptides in solution

Abstract

Exenatide, a polypeptide having the 39 amino acid sequence H-1His-Gly-Glu-Gly-5Thr-Phe-Thr-Ser-Asp-10Leu-Ser-Lys-Gln-Met-15Glu-Glu-Glu- -Ala-Val-20Arg-Leu-Phe-lle-Glu-25Trp-Leu-Lys-Asn-Gly-30Gly-Pro-Ser-Ser-Gly-35Ala- -Pro-Pro-Pro-Ser-NH2, respectively its 44-mer analogue H-1His-Gly-Glu-Gly-5Thr-Phe-Thr-Ser-Asp-10Leu-Ser-Lys-Gln-Met-15Glu-Glu-Glu- -Ala-Val-20Arg-Leu-Phe-lle-Glu-25Trp-Leu-Lys-Asn-Gly-30Gly-Pro-Ser-Ser-Gly-35Ala- -Pro-Pro-Ser-Lys-40Lys-Lys-Lys-Lys-Lys-NH2 is prepared via a convergent four-fragment synthesis strategy from the fragments comprising the amino acid positions 1-10, 11-21, 22-29 and 30-39, respectively 30-44.

IPC Classes  ?

• C07K 1/02 - General processes for the preparation of peptides in solution
• C07K 14/575 - Hormones

Abstract

The present invention relates to a process for the production of bivalirudin, a 20-mer peptide of formula H-D-Phe1-Pro-Arg-Pro-Gly5-Gly-Gly-Gly-Asn-Gly10-Asp-Phe-Glu-Glu-lle15- -Pro-Glu-Glu-Tyr-Leu20-OH (I) via a convergent five-fragment synthesis, and to several peptide intermediates thereof.

IPC Classes  ?

• C07K 5/10 - Tetrapeptides
• C07K 14/815 - Protease inhibitors from leeches, e.g. hirudin, eglin