Aryl thiol compound as well as preparation method and application thereof

• Main Authors: TIAN CHANGLIN, WANG MIAO, SHEN XINGYI, LIANG JUN, YAN CHENGJUN
• Format: Patent
• Language: Chinese; English
• Published: 29.03.2024
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES

The invention provides an aryl thiol compound as well as a preparation method and application thereof. The aryl thiol compound is a compound as shown in a formula (III), and a stereoisomer, a tautomer, a hydrate and a solvate of the aryl thiol compound, and the compound can be used for carrying out in-situ thiolysis on activated hydrazide and o-phenylenediamine into aryl thioester and is used for natural chemical connection between a polypeptide thioester peptide fragment and a peptide fragment with the N end modified by cysteine. And the reaction kinetics is high. According to the method, 4-mercaptophenylacetic acid is modified, so that the problems of precipitation and aggregation caused by loss of a C-terminal hydrotropy label in a natural chemical connection process of a hydrophobic peptide fragment can be solved, and the natural chemical connection efficiency of a polypeptide intermediate is improved. # imgabs0 # 本发明提供了一种芳基硫醇化合物及其制备方法和用途。所述芳基硫醇化合物为式(III)所示化合物、及其立体异构体、互变异构体、水合物、溶剂化物，该化合物可将活化的酰肼以及邻苯二胺原位硫解为