{"created":"2023-05-15T14:38:18.708021+00:00","id":49439,"links":{},"metadata":{"_buckets":{"deposit":"d1483acb-701f-4283-951a-de15cc03334d"},"_deposit":{"created_by":1,"id":"49439","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"49439"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00049439","sets":["1"]},"author_link":["909094","909091","909093","909095","909100","909092","909099","909090","909096","909097","909098","909089"],"item_8_biblio_info_7":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2019-01","bibliographicIssueDateType":"Issued"},"bibliographicPageEnd":"171","bibliographicPageStart":"165","bibliographicVolumeNumber":"17","bibliographic_titles":[{"bibliographic_title":"Organic & Biomolecular Chemistry"}]}]},"item_8_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"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.","subitem_description_type":"Abstract"}]},"item_8_publisher_8":{"attribute_name":"出版者","attribute_value_mlt":[{"subitem_publisher":"The Royal Society of Chemistry"}]},"item_8_relation_14":{"attribute_name":"DOI","attribute_value_mlt":[{"subitem_relation_type_id":{"subitem_relation_type_id_text":"10.1039/c8ob02394h","subitem_relation_type_select":"DOI"}}]},"item_access_right":{"attribute_name":"アクセス権","attribute_value_mlt":[{"subitem_access_right":"metadata only access","subitem_access_right_uri":"http://purl.org/coar/access_right/c_14cb"}]},"item_creator":{"attribute_name":"著者","attribute_type":"creator","attribute_value_mlt":[{"creatorNames":[{"creatorName":"Watanabe, Shigeki"}],"nameIdentifiers":[{"nameIdentifier":"909089","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Mohammad, Anwar-Ul Azim (Bangladesh Atomic Energy Commission)"}],"nameIdentifiers":[{"nameIdentifier":"909090","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Nishinaka, Ichiro"}],"nameIdentifiers":[{"nameIdentifier":"909091","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Sasaki, Ichiro"}],"nameIdentifiers":[{"nameIdentifier":"909092","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Oshima, Yasuhiro"}],"nameIdentifiers":[{"nameIdentifier":"909093","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Keiichi, Yamada (Gunma Univ.)"}],"nameIdentifiers":[{"nameIdentifier":"909094","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ishioka, Noriko"}],"nameIdentifiers":[{"nameIdentifier":"909095","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Watanabe, Shigeki","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"909096","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Nishinaka, Ichiro","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"909097","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Sasaki, Ichiro","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"909098","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Oshima, Yasuhiro","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"909099","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ishioka, Noriko","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"909100","nameIdentifierScheme":"WEKO"}]}]},"item_language":{"attribute_name":"言語","attribute_value_mlt":[{"subitem_language":"eng"}]},"item_resource_type":{"attribute_name":"資源タイプ","attribute_value_mlt":[{"resourcetype":"journal article","resourceuri":"http://purl.org/coar/resource_type/c_6501"}]},"item_title":"A convenient and reproducible method for the synthesis of astatinated 4-[211At]astato-L-phenylalanine via electrophilic desilylation","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"A convenient and reproducible method for the synthesis of astatinated 4-[211At]astato-L-phenylalanine via electrophilic desilylation"}]},"item_type_id":"8","owner":"1","path":["1"],"pubdate":{"attribute_name":"公開日","attribute_value":"2018-12-07"},"publish_date":"2018-12-07","publish_status":"0","recid":"49439","relation_version_is_last":true,"title":["A convenient and reproducible method for the synthesis of astatinated 4-[211At]astato-L-phenylalanine via electrophilic desilylation"],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-15T21:06:02.661142+00:00"}