Abstract: The invention discloses a method for the preparation of a peptide by liquid phase coupling of two fragments, an N-terminal fragment and a C-terminal fragment of the desired peptide, wherein the C-terminal fragment is protected on its C-terminal COOH by a psWang linker; the method is demonstrated with liraglutide wherein the C-terminal fragment carries the Palmitoyl-Glu-OtBu residue on the Lys.

Abstract: The invention discloses a method for the preparation of a peptide by liquid phase coupling of two fragments, an N-terminal fragment and a C-terminal fragment of the desired peptide, wherein the C-terminal fragment is protected on its C-terminal COOH by a psWang linker; the method is demonstrated with liraglutide wherein the C-terminal fragment carries the Palmitoyl-Glu-OtBu residue on the Lys.

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-Ile15-Pro-Glu-Glu-Tyr-Leu20-OH ??(I) via a convergent five-fragment synthesis, and to several peptide intermediates thereof.

Abstract: The present invention relates to a process for the production of bivalirudin, a 20-mer peptide of formula H-(D)-Phe-Pro-Arg-Pro-Gly-Gly-Gly-Asn-Gly-Asp-Phe-Glu-Glu-Ile-Pro-Glu-Glu-Tyr-Leu-OH (SEQ ID NO: 1).

Abstract: 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 includes a step a) and a step b): step a) including 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) including the subsequent separation of the organic layer containing the peptide from the aqueous layer. In an embodiment, 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.

Abstract: 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 N,N-dimethylformamide, N,N-dimethylacetamide and N-methyl-2-pyrrolidone, whereby the process includes a step a) and a step b): step a) including 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) including the subsequent separation of the organic layer containing the peptide from the aqueous layer. In an embodiment, a combination of toluene and an organic solvent 1 selected from 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.

Abstract: 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 N,N-dimethylformamide, N,N-dimethylacetamide and N-methyl-2-pyrrolidone, whereby the process includes a step a) and a step b): step a) including 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 2-methyltetrahydrofuran and toluene, component a2) is water, and component a3) is an organic solvent 2, the organic solvent 2 is selected from the 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) including the subsequent separation of the organic layer containing the peptide from the aqueous layer.

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-Ile14-Pro-Glu-Glu-Tyr-Lee-OH (I) via a convergent five-fragment synthesis, and to several peptide intermediates thereof.

Abstract: The present invention provides, inter alia, convergent processes for preparing eptifibatide that involve coupling a 2-6 eptifibatide fragment to an activated cysteinamide residue to form a 2-7 eptifibatide fragment, attaching a mercaptopropionic acid residue to the 2-7 eptifibatide fragment through disulfide bond formation, coupling the peptide intramolecularly, and removing the protecting group, to form eptifibatide. The invention further provides products produced by the described processes, novel compounds that can be used as synthetic intermediates for the preparation of eptifibatide, and novel compounds that are structurally similar to eptifibatide.

Abstract: The present invention provides, inter alia, convergent processes for preparing eptifibatide that involve coupling a 2-6 eptifibatide fragment to an activated cysteinamide residue to form a 2-7 eptifibatide fragment, attaching a mercaptopropionic acid residue to the 2-7 eptifibatide fragment through disulfide bond formation, coupling the peptide intramolecularly, and removing the protecting group, to form eptifibatide. The invention further provides products produced by the described processes, novel compounds that can be used as synthetic intermediates for the preparation of eptifibatide, and novel compounds that are structurally similar to eptifibatide.

Abstract: The present invention relates to an improved process for supported phase synthesis, in particular for supported phase peptide synthesis, that makes use of salts, in particular of quaternary ammonium salts.

Abstract: The present invention provides, inter alia, convergent processes for preparing eptifibatide that involve coupling a 2-6 eptifibatide fragment to an activated cysteinamide residue to form a 2-7 eptifibatide fragment, attaching a mercaptopropionic acid residue to the 2-7 eptifibatide fragment through disulfide bond formation, coupling the peptide intramolecularly, and removing the protecting group, to form eptifibatide. The invention further provides products produced by the described processes, novel compounds that can be used as synthetic intermediates for the preparation of eptifibatide, and novel compounds that are structurally similar to eptifibatide.

Abstract: This invention relates to new derivatives of 1-amino-fluoren-9-one and to the use thereof, particularly as herbicides.The new derivatives are 1-amino-fluoren-9-ones substituted in position 1 by a dialkylamino radical or a nitrogenous heterocyclic ring and possibly also substituted in at least one other position by a halogen atom, a trihalogenomethyl radical, a trifluoromethylsulfonyl radical and/or a nitro radical.