Yu Weijiang, Yang Yuqi, Bo Shaowei, Li Yu, Chen Shizhen, Yang Zhigang, Zheng Xing, Jiang Zhong-Xing, Zhou Xin
†Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (Wuhan University), Ministry of Education and Wuhan University School of Pharmaceutical Sciences, Wuhan 430071, China.
‡Key Laboratory of Magnetic Resonance in Biological Systems, State Key Laboratory for Magnetic Resonance and Atomic and Molecular Physics, National Center for Magnetic Resonance in Wuhan, Wuhan Institute of Physics and Mathematics, Chinese Academy of Sciences, Wuhan 430071, China.
J Org Chem. 2015 May 1;80(9):4443-9. doi: 10.1021/acs.joc.5b00294. Epub 2015 Apr 20.
To achieve high sensitivity for (19)F MRI, a class of novel dendritic molecules with multiple pseudosymmetrical fluorines was designed and efficiently synthesized. Through iterative bromination and Williamson ether synthesis under mild conditions, a fluorinated dendrimer with 540 pseudosymmetrical fluorines was conveniently prepared without performing the group protection in a convergent way. The dendrimer is characterized by a strong (19)F NMR peak and short relaxation times. Eventually, an appreciably enhanced (19)F MRI at an extremely low concentration (18.5 μM) was achieved, which demonstrated the potential utility of such dendritic molecules in highly sensitive (19)F MRI.
为实现高灵敏度的¹⁹F磁共振成像（MRI），设计并高效合成了一类具有多个伪对称氟原子的新型树枝状分子。通过在温和条件下进行迭代溴化反应和威廉姆森醚合成反应，简便地制备了一种含有540个伪对称氟原子的氟化树枝状大分子，无需采用收敛法进行基团保护。该树枝状大分子的特征在于具有较强的¹⁹F核磁共振（NMR）峰和较短的弛豫时间。最终，在极低浓度（18.5 μM）下实现了¹⁹F MRI的显著增强，这证明了此类树枝状分子在高灵敏度¹⁹F MRI中的潜在应用价值。
