Method for preparing CW7213 by polypeptide solid-phase synthesis

Abstract

The invention provides a method for preparing CW7213 by polypeptide solid-phase synthesis, which comprises the following steps of: with Fmoc-Gly-WANG resin as an initial raw material, Fmoc protected amino acid as a monomer and HBTU (Benzotriazole-N,N,N'N'-hexafluorophosphate) / HoBT (1-Hydroxybenzotrizole) as a condensing agent, charging nitrogen in a sand core funnel for gradually connecting amino acids to obtain protected 24 peptide resin; removing Fmoc protecting groups in sequence; synchronously removing side chain protecting groups and cutting peptide and adding diethyl ether for sedimenting to obtain a crude product of CW7213; subjecting the crude product to separation and purification by a C18 column; and carrying out freezing and drying to obtain a product (comprising medically available salts, such as acetate, trifluoroacetate, and the like). The method provided by the invention has the advantages of stable and mature process, convenience of raw and auxiliary material sources, high peptide yield, less pollution and convenience in industrialized construction and can avoid the use of virulent reagents, such as hydrogen fluoride, and the like.

Description

technical field [0001] The invention relates to a preparation method of CW7213, in particular to a preparation method of solid-phase polypeptide synthesis of CW7213. Background technique [0002] Chinese name: Insulin Release-Promoting Peptide from Fingerless Frog [0003] Abbreviation: CW7213 [0004] Isoelectric point: 10.32 [0005] Molecular weight: 2632.3 [0006] Structural formula: Phe-Leu-Pro-Leu-Leu-Ala-Gly-Leu-Ala-Ala-Asn(Trt)-Phe-Leu-Pro-Lys(boc)-Leu-Phe-Cys(trt)-Lys(boc )-Ile-Thr(tbu)-Arg(pbf)-Lys(boc)-Gly-OH [0007] Diabetes mellitus is a syndrome characterized by persistent hyperglycemia as the basic biochemical feature. A variety of reasons cause relative or absolute lack of insulin and different degrees of insulin resistance, making carbohydrate, fat and protein metabolism disorder, clinically manifested as diabetes. As the course of the disease prolongs, extensive microvascular and macrovascular lesions may appear, leading to blindness, renal failure,...

AI Technical Summary

Problems solved by technology

[0010] Traditional peptide synthesis methods are mostly liquid-phase synthesis or solid-phase boc strategy synthesis. Due to the serious process wastes and the use of highly toxic hydrogen fluoride, the efficiency of peptide incorporation is low, the reaction time is long, the process is complicated, and the product yield is low. It does not have the ability of large-scale production, and the preparation process of CW7213 has not been reported yet