Nucleophilic radiosynthesis of boron neutron capture therapy-oriented PET probe [18F]FBPA using aryldiboron precursors

Jing He; Heng Yan; Yanrong Du; Yan Ji; Fei Cai; Wenbin Fan; Li Huo; Yuan-Hao Liu; Zheng Wang; Shihong Li

doi:10.1039/d1cc03369g

Nucleophilic radiosynthesis of boron neutron capture therapy-oriented PET probe [¹⁸F]FBPA using aryldiboron precursors

Chem Commun (Camb). 2021 Sep 6;57(71):8953-8956. doi: 10.1039/d1cc03369g.

Authors

Jing He¹, Heng Yan², Yanrong Du³, Yan Ji², Fei Cai^{2

4}, Wenbin Fan², Li Huo³, Yuan-Hao Liu^{1

4}, Zheng Wang², Shihong Li^{2

5}

Affiliations

¹ Neuboron Medtech Ltd., No. 568 Longmian Ave, 211100, Nanjing, P. R. China.
² JYAMS PET Research and Development Limited, No. 568 Longmian Ave, Nanjing, 211100, P. R. China. lishhchem@126.com.
³ Department of Nuclear Medicine, Peking Union Medical College Hospital, Chinese Academy of Medical Sciences and Peking Union Medical College, No. 1 Shuaifuyuan, Wangfujing Street, Beijing, 100730, P. R. China. duyr@pumch.cn.
⁴ Department of Nuclear Sciences and Engineering, Nanjing University of Aeronautics and Astronautics, 29 Yudao Street, Nanjing, 210016, P. R. China.
⁵ State Key Laboratory of Radiation Medicine and Protection, School of Radiation Medicine and Protection, Soochow University, No. 199 Ren'ai Road, Suzhou Industrial Park, Suzhou, Jiangsu, 215123, P. R. China.

PMID: 34486586
DOI: 10.1039/d1cc03369g

Abstract

A reliable copper-mediated nucleophilic radiosynthesis of the PET imaging probe [¹⁸F]FBPA was developed using novel aryldiboron precursors. The carrier-free [¹⁸F]FBPA with radiochemical purity >99% was prepared routinely via the two-step synthesis with an automatic module and can be used for clinical PET imaging of tumours.

MeSH terms

Animals
Boron Compounds / chemical synthesis
Boron Compounds / chemistry*
Fluorine Radioisotopes / chemistry
Phenylalanine / analogs & derivatives*
Phenylalanine / chemical synthesis
Positron-Emission Tomography
Radiopharmaceuticals / chemical synthesis
Radiopharmaceuticals / chemistry*

Substances

Boron Compounds
Fluorine Radioisotopes
Radiopharmaceuticals
Phenylalanine
Fluorine-18