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†

Jing He,^a Heng Yan,^b Yanrong Du,*^c Yan Ji,^b Fei Cai,

^bd Wenbin Fan,^b Li Huo,^c Yuan-Hao Liu,^ad Zheng Wang^b and Shihong Li

*^be

Author affiliations

* Corresponding authors

^a Neuboron Medtech Ltd., No. 568 Longmian Ave, Nanjing, P. R. China

^b JYAMS PET Research and Development Limited, No. 568 Longmian Ave, Nanjing, P. R. China
E-mail: lishhchem@126.com

^c 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, P. R. China
E-mail: duyr@pumch.cn

^d Department of Nuclear Sciences and Engineering, Nanjing University of Aeronautics and Astronautics, 29 Yudao Street, Nanjing, P. R. China

^e 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, P. R. China

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.

Chemical Communications

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

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

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