Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals and School of Pharmaceutical Sciences, Wuhan University, Wuhan 430071, China.
State Key Laboratory of Magnetic Resonance and Atomic and Molecular Physics, National Center for Magnetic Resonance in Wuhan, Wuhan Institute of Physics and Mathematics, Innovative Academy of Precision Measurement Science and Technology, Chinese Academy of Sciences, Wuhan 430071, China.
J Org Chem. 2020 May 15;85(10):6778-6787. doi: 10.1021/acs.joc.0c00331. Epub 2020 May 7.
Multifunctionalized and branched M-OEGs represent valuable PEGylation agents, linkers, and scaffolds in biomedicine. However, the tedious synthesis limited their availability and application. We herein present an azide reductive dimerization method for the convenient synthesis of aza-M-OEGs and derivatives, which provides easy access to a variety of multifunctionalized and branched M-OEGs in one step. With this method, hexa-arm M-OEGs with 54 symmetrical fluorines were synthesized in two steps as a water-soluble, self-assemble, F MRI sensitive, and biocompatible dendritic biomaterial.
多功能化和支化的 M-OEG 代表了有价值的 PEGylation 试剂、连接子和生物医学中的支架。然而，繁琐的合成限制了它们的可用性和应用。在此，我们提出了一种叠氮化物还原二聚化方法，用于方便合成氮杂 M-OEGs 和衍生物，该方法可在一步中轻松获得各种多功能化和支化的 M-OEG。通过这种方法，以两步法合成了具有 54 个对称氟原子的六臂 M-OEG，其为水溶性的、自组装的、F MRI 敏感的和生物相容的树枝状生物材料。
