| Item type |
学術雑誌論文 / Journal Article(1) |
| 公開日 |
2024-03-04 |
| タイトル |
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タイトル |
Copper-mediated astatination of 211At-labelled prostate-specific membrane antigen probes in the presence of basic salts |
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言語 |
en |
| 言語 |
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|
言語 |
eng |
| 資源タイプ |
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資源タイプ識別子 |
http://purl.org/coar/resource_type/c_6501 |
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資源タイプ |
journal article |
| 著者 |
Watanabe Shigeki
Yuto Kondo (KPU)
Sasaki Ichiro
Oshima Yasuhiro
Hiroyuki Kimura (Kanazawa Univ)
Ishioka Noriko
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| 抄録 |
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内容記述タイプ |
Abstract |
|
内容記述 |
Highly toxic alpha emitting radionuclide, astatine-211 (211At) labelled compounds have great potential as therapeutic radiopharmaceuticals in the targeted alpha therapy (TAT). Previously we have reported the usefulness of copper (Cu)-mediated radiobromination and radioiodination via boronic acid precursors for the synthesis of 77Br/125I-labelled prostate-specific membrane antigen (PSMA) inhibitors which are applicable as imaging probes. This background led us to investigate the Cu-mediated astatination of PSMA inhibitors as a therapeutic agent for TAT. 211At-labelled PSMA inhibitors [211At]mAtB-PS were synthesised from a boronic acid precursor with tert-butoxycarbonyl groups by Cu-mediated astatination in the presence or absence of NaOH and K2CO3 in order to stabilize the chemical form of At followed by deprotection of the tert-butoxycarbonyl group under acidic condition. We confirmed that [211At]mAtB-PS 1a was synthesised in 64.4?87.3% of overall radiochemical yields (RCYs). These yields are considered acceptable regardless of basic salts existed. However, RCYs of the astatination step differed depending on the base (NaOH: 22.0?31.9%; K2CO3; 69.0?82.3%; without base: 60.1%). We speculated that astatination also occurred during the deprotection of tert-butoxycarbonyl groups. This could be attributed to an electrophilic deboronation reaction involving electrophilic astatine species, resulting in compensation for the overall RCYs. Cu-mediated astatination via boronic precursors was found to be very effective for the synthesis of 211At-labelled PSMA inhibitors for the targeted alpha therapy. |
| 書誌情報 |
Tetrahedron
発行日 2024-03
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| 出版者 |
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出版者 |
Elsevir |
