C07K1/08

REACTION AGENT FOR AMIDE REACTIONS AND AMIDE COMPOUND PRODUCTION METHOD USING SAME
20230002422 · 2023-01-05 ·

[Problem] To provide a novel means capable of generating highly stereoselective and/or highly efficient amidation reactions in a variety of substrates having a carboxyl group and an amino group, and capable of producing amide compounds.

[Solution] A reaction agent for amide reactions between carboxyl groups and amino groups and including a silane compound indicated by general formula (A) and/or general formula (B).

##STR00001##

(In general formulas (A) and (B), each substituent represents the definition described in the Claims.)

Method for producing amide compound

Provided is a novel method whereby an amide compound can be produced by highly stereoselectively and efficiently performing amidation between a plurality of amino acids and/or peptides. A compound of general formula (3) is synthesized by forming an amide bond between the carboxyl group on the right side of general formula (1) in a compound represented thereby and the amino group on the left side of general formula (2) in a compound represented thereby, in the presence of a Lewis acid catalyst and a silylating agent [in formulae (1), (2) and (3), each symbol has the same meaning as defined in claims]. ##STR00001##

Method for producing amide compound

Provided is a novel method whereby an amide compound can be produced by highly stereoselectively and efficiently performing amidation between a plurality of amino acids and/or peptides. A compound of general formula (3) is synthesized by forming an amide bond between the carboxyl group on the right side of general formula (1) in a compound represented thereby and the amino group on the left side of general formula (2) in a compound represented thereby, in the presence of a Lewis acid catalyst and a silylating agent [in formulae (1), (2) and (3), each symbol has the same meaning as defined in claims]. ##STR00001##

Peptoid compound and manufacturing method thereof, oligomer, pharmaceutical composition, and kit

A peptoid compound, a manufacturing method of a peptoid compound, an oligomer, a pharmaceutical composition, use of the pharmaceutical composition in the preparation of a medicament for detecting or diagnosing a disease related to tyrosine kinase HER2, and a kit for identifying circulating tumor cells are provided, the peptoid compound includes: a cysteine (Cys) subunit, a butanediamine (Nlys) subunit, a 3,4-methylenedioxybenzylamine (Npip) subunit, a 3-aminopropanic acid (Nce) subunit and a 1-naphthylamine (Na) subunit, and both the peptoid compound and the oligomer have a strong ability to bind to HER2 protein on surfaces of circulating tumor cells (CTCs), and a technology of diagnosing breast cancer on the basis of the peptoid compound can realize non-invasive and label-free rapid diagnosis, in addition, the methods for synthesizing the peptoid compound and the oligomer are simple, the preparation efficiency is high, and the production cost is low.

Peptoid compound and manufacturing method thereof, oligomer, pharmaceutical composition, and kit

A peptoid compound, a manufacturing method of a peptoid compound, an oligomer, a pharmaceutical composition, use of the pharmaceutical composition in the preparation of a medicament for detecting or diagnosing a disease related to tyrosine kinase HER2, and a kit for identifying circulating tumor cells are provided, the peptoid compound includes: a cysteine (Cys) subunit, a butanediamine (Nlys) subunit, a 3,4-methylenedioxybenzylamine (Npip) subunit, a 3-aminopropanic acid (Nce) subunit and a 1-naphthylamine (Na) subunit, and both the peptoid compound and the oligomer have a strong ability to bind to HER2 protein on surfaces of circulating tumor cells (CTCs), and a technology of diagnosing breast cancer on the basis of the peptoid compound can realize non-invasive and label-free rapid diagnosis, in addition, the methods for synthesizing the peptoid compound and the oligomer are simple, the preparation efficiency is high, and the production cost is low.

SITE-SPECIFIC CONJUGATION THROUGH GLYCOPROTEINS LINKAGE AND METHOD THEREOF

A method for specific linkage to a glycoprotein includes obtaining a glycoprotein having a monoglycan or diglycan attached thereto; producing a reactive functional group on a sugar unit on the glycoprotein; and coupling a linker or a payload to the reactive functional group on the glycoprotein.

SITE-SPECIFIC CONJUGATION THROUGH GLYCOPROTEINS LINKAGE AND METHOD THEREOF

A method for specific linkage to a glycoprotein includes obtaining a glycoprotein having a monoglycan or diglycan attached thereto; producing a reactive functional group on a sugar unit on the glycoprotein; and coupling a linker or a payload to the reactive functional group on the glycoprotein.

COUPLING METHOD FOR PEPTIDE SYNTHESIS AT ELEVATED TEMPERATURES
20170342104 · 2017-11-30 · ·

An improved method for coupling amino acids into peptides or peptidomimetics is disclosed that includes the steps of combining an amino acid, a carbodiimide, an activator additive, and a base at less than 1 equivalent compared to the amino acid to be activated; and carrying out the activation and coupling at a temperature greater than 30° C.

COUPLING METHOD FOR PEPTIDE SYNTHESIS AT ELEVATED TEMPERATURES
20170342104 · 2017-11-30 · ·

An improved method for coupling amino acids into peptides or peptidomimetics is disclosed that includes the steps of combining an amino acid, a carbodiimide, an activator additive, and a base at less than 1 equivalent compared to the amino acid to be activated; and carrying out the activation and coupling at a temperature greater than 30° C.

SOLID PHASE PEPTIDE SYNTHESIS METHODS AND ASSOCIATED SYSTEMS

Methods and system for solid phase peptide synthesis are provided. Solid phase peptide synthesis is a known process in which amino acid residues are added to peptides that have been immobilized on a solid support. New amino acid residues are added via a coupling reaction between an activated amino acid and an amino acid residue of the immobilized peptide. Amino acids may be activated using, e.g., a base and an activating agent. Certain inventive concepts, described herein, relate to methods and systems for the activation of amino acids. These systems and methods may allow for fewer side reactions and a higher yield compared to conventional activation techniques as well as the customization of the coupling reaction on a residue-by-residue basis without the need for costly and/or complex processes.