The chemical synthesis of polypeptide synthesis is divided into two methods, liquid phase synthesis and solid phase synthesis, depending on whether or not a solid phase carrier is used. Glucose Test Strips,Best Blood Glucose Meter,Blood Sugar Test Machine,Glucose Monitoring System Wuxi BioHermes Bio & Medical Technology Co., Ltd. , https://www.biohermesglobal.com
1 Liquid phase synthesis of peptide drugs: The liquid phase synthesis of peptides is mainly carried out in liquids, so it is called liquid phase synthesis method, and there are two strategies of stepwise synthesis and fragment combination. The stepwise synthesis is simple and rapid, and is used for the synthesis of various biologically active polypeptide fragments. The fragment combination method provides the most promising route for polypeptide synthesis, and has successfully synthesized a variety of biologically active polypeptides, the most important feature of which is easy to be pure system.
For polypeptides composed of fewer amino acids, liquid phase synthesis is convenient, rapid, high purity, and capable of large-scale synthesis. Sun Yongqiang et al. used Fmoc as a side chain amino acid protecting group to gradually synthesize the decapeptide triptorelin, and the synthesized triptorelin has a higher yield. The functionalized ionic liquid as the carrier liquid phase synthesis technology has obvious advantages in the peptide synthesis reaction: the selectivity, speed and yield of the reaction are significantly improved, the reaction after the reaction is convenient, and the ionic liquid can be recycled and used. Xu Zhongyi et al. successfully synthesized the RGD tripeptide with a functionalized ionic liquid as the carrier, and the target compound did not require further chromatographic purification, and the yield was 84%. In addition, the study also found that some amino acids are modified and prepared by liquid phase synthesis of peptide drugs after being modified by acid-resistant and easily cleavable hydrophobic groups. Okada et al. introduced a liquid phase synthesis of a polypeptide by using a benzyl alcohol hydrophobic group as an auxiliary support, and successfully synthesized a gram-grade leuprolide, bivalirudin, gastric somatotropin and other polypeptide drugs. The somatostatin----somatostatin was successfully synthesized by hydrophobic labeling assisted liquid phase synthesis.
2 Solid phase synthesis of peptide drugs: Solid phase synthesis is a method for synthesizing peptides by immobilizing the C-terminus of an amino acid on an insoluble resin and then sequentially condensing the amino acid on the resin. Since Merrifield developed the solid phase synthesis peptide synthesis in 1963, it has been continuously improved and perfected. Today, the solid phase method has become a common technique in the synthesis of peptides and proteins, showing the incomparable classical liquid phase synthesis. advantage. The a-amino group is protected by Boc (tert-butoxycarbonyl), which is called Boc solid phase synthesis, and the a-amino group is protected by Fmoc (9-fluorenylmethoxycarbonyl), which is called Fmoc solid phase synthesis.
Nowadays, solid phase synthesis has been widely used in various fields of peptide synthesis, and solid phase synthesis is generally preferred for polypeptides of <30 amino acids. Shi Weihua et al. applied Fmoc solid phase synthesis method, RinkAmide-AMResin as carrier, DIC/ HOBt or DIC/HOAt as condensing agent, and purified by preparative reversed-phase high performance liquid chromatography. The purity was as high as 99%. The rate is 62% of cetrorelixin. Dixon et al. synthesized a chitinase inhibitor, arcifin, which is a cyclic pentapeptide by solid phase synthesis. The synthesis method is characterized by a protected aspartic acid before the arcifin is looped. (Asp) is first linked to a solid support, and then a linear peptide chain is formed by Fmoc solid phase synthesis to participate in the synthesis of the polypeptide. Afonso et al. introduced a boronic acid group into a side chain protecting group and combined with microwave-assisted Suzuki-Miyaura interaction to form a cyclic peptide, successfully synthesizing a biaryl cyclic peptide drug, the biaryl cyclic peptide drug It is characterized in that the amino acid at position 3 is substituted with 3-aryltyrosine in order to enable simple and efficient solid phase synthesis.
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