Thioester peptide synthesis method

• Main Authors: YU FEIQIANG, FANG GEMIN, YIN QINGHONG, XIE XIAOLEI
• Format: Patent
• Language: Chinese; English
• Published: 15.03.2022
• Subjects: CHEMISTRY; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES

The invention discloses a thioester peptide synthesis method, which specifically comprises the following steps: dissolving polypeptide hydrazide in a hydrochloric acid-containing mixed solvent consisting of dimethyl sulfoxide and water, and reacting with isoamyl nitrite in an ice-salt bath to generate acyl azide peptide; adding excessive methyl thioglycolate, and then adding ammonium bicarbonate prepared in advance to adjust the acidity of the solution to be neutral, so that the acyl azide peptide is converted into peptide thioester; pre-cooled trifluoroacetic acid and diethyl ether are sequentially added into a reaction system, so that thioester peptide is crystallized and separated. The thioester peptide is prepared through the low-cost, simple and rapid operation process, and the problem that high-cost high performance liquid chromatography and time-consuming freeze drying operation are needed in traditional thioester peptide synthesis is solved. 本发明公开了一种硫酯肽合成方法，具体工序包括：多肽酰肼溶解在含盐酸的由二甲基亚砜和水组成的混合溶剂中，在冰盐浴下与亚硝酸