Large-scale synthesis of Notum inhibitor 1-(2,4-dichloro-3-(trifluoromethyl)-phenyl)-1<i>H</i>-1,2,3-triazole (ARUK3001185) employing a modified Sakai reaction as the key step-Reference-Cited by-同舟云学术

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

Published:2022 Issue:41 Volume:12 Page:26497-26503
ISSN:2046-2069
Container-title:RSC Advances
language:en
Short-container-title:RSC Adv.

Author:

Atkinson Benjamin N.¹^ORCID,Willis Nicky J.¹^ORCID,Smith Jennifer²,Gill Rebecca²,Ali Jody²,Xu Zhou³,Lai Ping-Shan³,Fish Paul V.¹^ORCID

Affiliation:

1. Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London, WC1E 6BT, UK

2. Key Organics Ltd, Highfield Road Industrial Estate, Camelford, Cornwall, PL32 9RA, UK

3. WuXi AppTec (Tianjin) Co., Ltd., 168 Nanhai Road, 10th Avenue, Tianjin Economic-Technological Development Area (TEDA), Tianjin 300457, P.R. China

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.

Funder

Alzheimer's Drug Discovery Foundation

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemical Engineering,General Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2022/RA/D2RA05132J

Reference23 articles.

1. Wnt/β-Catenin Signaling, Disease, and Emerging Therapeutic Modalities

2. Notum deacylates Wnt proteins to suppress signalling activity

3. Notum Is Required for Neural and Head Induction via Wnt Deacylation, Oxidation, and Inactivation

4. NOTUM inhibition increases endocortical bone formation and bone strength

5. NOTUM from Apc-mutant cells biases clonal competition to initiate cancer

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