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Large-scale synthesis of Notum inhibitor 1-(2,4-dichloro-3-(trifluoromethyl)-phenyl)-1H-1,2,3-triazole (ARUK3001185) employing a modified Sakai reaction as the key step

Atkinson, Benjamin N; Willis, Nicky J; Smith, Jennifer; Gill, Rebecca; Ali, Jody; Xu, Zhou; Lai, Ping-Shan; (2022) Large-scale synthesis of Notum inhibitor 1-(2,4-dichloro-3-(trifluoromethyl)-phenyl)-1H-1,2,3-triazole (ARUK3001185) employing a modified Sakai reaction as the key step. RSC Advances , 12 (41) pp. 26497-26503. 10.1039/d2ra05132j. Green open access

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Abstract

1-Phenyl-1H-1,2,3-triazole 1 was prepared on large scale from aniline 4 by application of a one-pot Sakai–Clark reaction in good efficiency and high purity.

Type: Article
Title: Large-scale synthesis of Notum inhibitor 1-(2,4-dichloro-3-(trifluoromethyl)-phenyl)-1H-1,2,3-triazole (ARUK3001185) employing a modified Sakai reaction as the key step
Open access status: An open access version is available from UCL Discovery
DOI: 10.1039/d2ra05132j
Publisher version: https://doi.org/10.1039/d2ra05132j
Language: English
Additional information: This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Keywords: Science & Technology, Physical Sciences, Chemistry, Multidisciplinary, Chemistry, NITROGEN-CONTAINING HETEROCYCLES, ARYLATION
UCL classification: UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Brain Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Brain Sciences > UCL Queen Square Institute of Neurology > Department of Neuromuscular Diseases
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Brain Sciences > UCL Queen Square Institute of Neurology
URI: https://discovery.ucl.ac.uk/id/eprint/10156334
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