3-acyl-4-pyrone derivative as coupling reagent and application of 3-acyl-4-pyrone derivative in preparation of polypeptide and protein conjugate

• Main Authors: ZHAO YILU, YAO ZHUJUN, XI JIE, NONG KEYI
• Format: Patent
• Language: Chinese; English
• Published: 14.11.2023
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES

The invention belongs to the technical field of organic synthesis and protein modification, and particularly relates to a 3-acyl-4-pyrone derivative serving as a coupling reagent and application of the 3-acyl-4-pyrone derivative to preparation of polypeptide and protein conjugates. The 3-acyl-4-pyrone derivative can be chemically and selectively subjected to O-to-N insertion substitution reaction with lysine residues in a polypeptide or protein sequence quickly and efficiently under near-physiological conditions, so that coupling of polypeptide and protein is realized; the 3-acyl-4-pyrone derivative is simple in synthesis method, simple and convenient in modification operation on protein and novel in structure, no coherent report is reported to be applied to polypeptide and protein modification, and a new technology and a new mode are provided for various functional modifications of polypeptide and protein. 本发明属于有机合成及蛋白质修饰技术领域，特别涉及一种3-酰基-4-吡喃酮衍生物作为偶联试剂及其在制备多肽、蛋白质偶联物中的应用，该3-酰基-4-吡喃酮衍生物可以在近生理条件下快速高效地与多肽或蛋白质序列中的