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A convenient and reproducible method for the synthesis of astatinated 4-[211At]astato-L-phenylalanine via electrophilic desilylation
https://repo.qst.go.jp/records/49439
https://repo.qst.go.jp/records/494397d8cd1a3-063e-4bdc-8261-0f7bf29eb98d
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2018-12-07 | |||||
| タイトル | ||||||
| タイトル | A convenient and reproducible method for the synthesis of astatinated 4-[211At]astato-L-phenylalanine via electrophilic desilylation | |||||
| 言語 | ||||||
| 言語 | eng | |||||
| 資源タイプ | ||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
| 資源タイプ | journal article | |||||
| アクセス権 | ||||||
| アクセス権 | metadata only access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
| 著者 |
Watanabe, Shigeki
× Watanabe, Shigeki× Mohammad, Anwar-Ul Azim (Bangladesh Atomic Energy Commission)× Nishinaka, Ichiro× Sasaki, Ichiro× Oshima, Yasuhiro× Keiichi, Yamada (Gunma Univ.)× Ishioka, Noriko× Watanabe, Shigeki× Nishinaka, Ichiro× Sasaki, Ichiro× Oshima, Yasuhiro× Ishioka, Noriko |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | The 211At-labeled compound, 4-[211At]astato-L-phenylalanine, is one of the most promising amino acid derivatives for use in targeted alpha therapy (TAT) for various cancers. Electrophilic demetallation of a stannyl precursor is the most widely used approach for labeling biomolecules with 211At. However, the low acid-resistance of the stannyl precursor necessitates the use of an N- and C- terminus-protected precursor, which results in a low overall radiochemical yield (RCY) due to the multiple synthetic steps involved. In this study, a deprotected organosilyl compound, 4-triethylsilyl-L-phenylalanine, was employed for the direct synthesis of astatinated phenylalanines. 211At was separately recovered from the irradiated 209Bi target using chloroform (CHCl3) and N-chlorosuccinimide-methanol (NCS-MeOH) solution. The RCYs of 4-[211At]astato-L-phenylalanine obtained from the triethylsilyl precursor with the use of 211At, isolated in CHCl3 and NCS-MeOH solution, were 75% and 64% respectively. In both cases, the retention time of the 4-[211At]astato-L-phenylalanine was found to be about 20 min, which showed reasonable correlation with the retention time of non-radioactive 4-halo-L-phenylalanines (4-chloro-, 4-bromo-, and 4-iodo-L-phenylalanine). The one-step reaction examined in this study involved mild reaction conditions (70 °C) and a short time (10 min) compared to the other currently reported procedures for astatination. Electrophilic desilylation was found to be very effective for the labeling of aromatic amino acids with 211At. | |||||
| 書誌情報 |
Organic & Biomolecular Chemistry 巻 17, p. 165-171, 発行日 2019-01 |
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| 出版者 | ||||||
| 出版者 | The Royal Society of Chemistry | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1039/c8ob02394h | |||||
