{"id":4011,"date":"2023-10-18T12:01:25","date_gmt":"2023-10-18T10:01:25","guid":{"rendered":"https:\/\/www.m2olie.de\/?post_type=publications&#038;p=4011"},"modified":"2024-02-02T12:08:37","modified_gmt":"2024-02-02T11:08:37","slug":"cyclosifa-the-next-generation-of-silicon-based-fluoride-acceptors-for-positron-emission-tomography-pet","status":"publish","type":"publications","link":"https:\/\/www.m2olie.de\/en\/publications\/cyclosifa-the-next-generation-of-silicon-based-fluoride-acceptors-for-positron-emission-tomography-pet\/","title":{"rendered":"CycloSiFA: The Next Generation of Silicon-Based Fluoride Acceptors for Positron Emission Tomography (PET)"},"content":{"rendered":"\n<p class=\"wp-block-paragraph\">Mawick M, Jaworski C, Bittermann J, Iovkova L, Pu Y, W\u00e4ngler C, W\u00e4ngler B, Jurkschat K, Krause N, Schirrmacher R (2023) CycloSiFA: The Next Generation of Silicon-Based Fluoride Acceptors for Positron Emission Tomography (PET). <em>Angewandte Chemie International Edition, 62(50)<\/em>, e202309002. <a href=\"https:\/\/onlinelibrary.wiley.com\/doi\/10.1002\/anie.202309002\" target=\"_blank\" rel=\"noreferrer noopener\">DOI: 10.1002\/anie.202309002.<\/a><\/p>\n\n\n\n<h2 class=\"wp-block-heading\" id=\"d227934691\">Graphical Abstract<\/h2>\n\n\n\n<p class=\"wp-block-paragraph\">Cyclic azasilole derivatives undergo ring-opening with <sup>18<\/sup>F<sup>\u2013<\/sup> anions under mild conditions and with high radiochemical yield. They represent a novel class of Silicon Fluoride Acceptor systems (<em>Cyclo<\/em>SiFA) and hold great potential for convenient kit-like labelling procedures in different medicinal applications.<\/p>\n\n\n\n<figure class=\"wp-block-image\"><a href=\"https:\/\/onlinelibrary.wiley.com\/cms\/asset\/96945fbe-3fa3-4341-a1b4-0d9a2b331ca6\/anie202309002-toc-0001-m.jpg\" target=\"_blank\" rel=\"noreferrer noopener\"><img decoding=\"async\" src=\"https:\/\/onlinelibrary.wiley.com\/cms\/asset\/a073e64e-a8fb-4452-80a4-64def47b9562\/anie202309002-toc-0001-m.png\" alt=\"Description unavailable\" title=\"Description unavailable\" \/><\/a><\/figure>\n\n\n\n<h2 class=\"wp-block-heading\" id=\"d227934694\">Abstract<\/h2>\n\n\n\n<p class=\"wp-block-paragraph\">The ring-opening Si-fluorination of a variety of azasilole derivatives <em>cyclo<\/em>-1-(<em>i<\/em>Pr<sub>2<\/sub>Si)\u22124-X\u2212C<sub>6<\/sub>H<sub>3<\/sub>\u22122-CH<sub>2<\/sub>NR (<strong>4<\/strong>: R=2,6-<em>i<\/em>Pr<sub>2<\/sub>C<sub>6<\/sub>H<sub>3<\/sub>, X=H; <strong>4\u2009a<\/strong>: R=2,4,6-Me<sub>3<\/sub>C<sub>6<\/sub>H<sub>2<\/sub>, X=H; <strong>9<\/strong>: R=2,6-<em>i<\/em>Pr<sub>2<\/sub>C<sub>6<\/sub>H<sub>3<\/sub>, X=<em>t<\/em>BuMe<sub>2<\/sub>SiO; <strong>10<\/strong>: R=2,6-<em>i<\/em>Pr<sub>2<\/sub>C<sub>6<\/sub>H<sub>3<\/sub>, X=OH; <strong>13<\/strong>: R=2,6-<em>i<\/em>Pr<sub>2<\/sub>C<sub>6<\/sub>H<sub>3<\/sub>, X=HCCCH<sub>2<\/sub>O; <strong>22<\/strong>: R=2,6-<em>i<\/em>Pr<sub>2<\/sub>C<sub>6<\/sub>H<sub>3<\/sub>, X=<em>t<\/em>BuMe<sub>2<\/sub>SiCH<sub>2<\/sub>O) with different <sup>19<\/sup>F-fluoride sources was studied, optimized and the experience gained was used in a translational approach to create a straightforward <sup>18<\/sup>F-labelling protocol for the azasilole derivatives [<sup>18<\/sup>F]<strong>6<\/strong> and [<sup>18<\/sup>F]<strong>14<\/strong>. The latter constitutes a potential clickable <em>Cyclo<\/em>SiFA prosthetic group which might be used in PET tracer development using Cu-catalysed triazole formation. Based on our findings, <em>Cyclo<\/em>SiFA has the potential to become a new entry into non-canonical labelling methodologies for radioactive PET tracer development.<\/p>\n","protected":false},"featured_media":0,"comment_status":"open","ping_status":"closed","template":"","meta":{"footnotes":""},"categories":[],"class_list":["post-4011","publications","type-publications","status-publish","hentry"],"_links":{"self":[{"href":"https:\/\/www.m2olie.de\/en\/wp-json\/wp\/v2\/publications\/4011","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/www.m2olie.de\/en\/wp-json\/wp\/v2\/publications"}],"about":[{"href":"https:\/\/www.m2olie.de\/en\/wp-json\/wp\/v2\/types\/publications"}],"replies":[{"embeddable":true,"href":"https:\/\/www.m2olie.de\/en\/wp-json\/wp\/v2\/comments?post=4011"}],"version-history":[{"count":1,"href":"https:\/\/www.m2olie.de\/en\/wp-json\/wp\/v2\/publications\/4011\/revisions"}],"predecessor-version":[{"id":4012,"href":"https:\/\/www.m2olie.de\/en\/wp-json\/wp\/v2\/publications\/4011\/revisions\/4012"}],"wp:attachment":[{"href":"https:\/\/www.m2olie.de\/en\/wp-json\/wp\/v2\/media?parent=4011"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/www.m2olie.de\/en\/wp-json\/wp\/v2\/categories?post=4011"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}