Liquid-phase synthetic method of E75 peptide

Abstract

The invention discloses a liquid-phase synthetic method of E75 peptide. The method comprises the steps of respectively synthesizing three peptide fragments, namely Boc-Lys-Ile-Phe-OH, NH2-Gly-Ser(t-BPS)-Leu-OCH3 and NH2-Ala-Phe-Leu-OCH3 of E75 peptide, and sequentially condensing the three peptide fragments, so as to obtain the E75 peptide. According to the liquid-phase synthetic method of the E75 peptide, intermediates in each step of the reaction process can be controlled one by one, so that the disadvantages of large impurity content and high purification and separation requirements in solid-phase synthesis of a final product are overcome. The method is simple in operation, the protection strategy controllability of adopted Boc and methoxy groups is very strong, the reaction yield of each step is relatively high, the product is easily separated and purified, and the purity of the final product can reach above 97%; and meanwhile, the industrial production of the E75 peptide is easily realized, the batch product is easily amplified, and the kilogram-level preparation can be realized in a pilot phase.

Description

technical field [0001] The invention relates to the field of polypeptide synthesis, in particular to a liquid phase synthesis method of E75 peptide. Background technique [0002] Breast cancer is the most common cancer in women and the second leading cause of cancer-related death in women. Major advances in breast cancer treatment over the past 20 years have resulted in significant improvements in disease-free survival (DFS) rates. For example, therapy using antibodies reactive to tumor-associated antigens has been used to block specific cellular processes to slow disease progression or prevent disease recurrence. Although recent progress has been made in the treatment of breast cancer, the recurrence rate and metastasis rate of breast cancer are relatively high because the current treatment methods for breast cancer cannot effectively eradicate the remaining cancer cells. Said to face a more complex and intractable problem. [0003] Theoretically, immunotherapy can compl...

AI Technical Summary

Problems solved by technology

Solid-phase synthesis has its significant advantages, such as simple operation and accelerated multi-step synthesis; however, the main problem of solid-phase synthesis is that each step of reaction requires the use of protected amino acids, and intermediate impurities on the solid-phase carrier cannot be separated, which leads to the final The product contains more impurities and has higher requirements for separation and purification, which increases the production cost

The output of solid-phase synthesis is generally not too high, and industrial production is not convenient

Images