Isotopic labeling reagent for amino/phenolic hydroxyl labeling and synthesis method thereof

• Main Authors: LIU MIN, HU YUFENG, WU MINGHUO, ZHOU HAO, LIU LIFEN, ZHAO KAIYONG
• Format: Patent
• Language: Chinese; English
• Published: 09.01.2018
• Subjects: APPARATUS THEREFOR; CHEMISTRY; GENERAL METHODS OF ORGANIC CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

The invention relates to one group of isotopic labeling reagent for amino/phenolic hydroxyl labeling and a synthesis method thereof. In a synthesis process, a reagent (such as a homologous compound of6-aminohexanoic acid) which simultaneously carries amino and carboxyl is used as a raw material and reacts with isotope D-containing or 13C substituted iodomethane or formaldehyde, so as to transformthe amino into quaternary ammonium and introduce an isotope on the iodomethane or the formaldehyde onto methyl of the quaternary ammonium. By selecting different D substituted or 13C substituted iodomethane and formaldehyde and regulating a reaction route, a series of products, which are substituted by different isotopes, can be obtained. The series of products further react with N-hydroxysuccinimide, so that the carboxyl and the hydroxyl of the N-hydroxysuccinimide react to form an ester, and one group of isotopic labeling reagent, which can efficiently react with the amino or the phenolic hydroxyl, is obtained. 本发明涉