An improved, scalable synthesis of Notum inhibitor LP-922056 using 1-chloro-1,2-benziodoxol-3-one as a superior electrophilic chlorinating agent

An improved, scalable synthesis of Notum inhibitor LP-922056 using 1-chloro-1,2-benziodoxol-3-one as a superior electrophilic chlorinating agent

Background: The carboxylesterase Notum has been shown to act as a key negative regulator of the Wnt signalling pathway by mediating the depalmitoleoylation of Wnt proteins. LP-922056 (1) is an orally active inhibitor of Notum. We are investigating the role of Notum in modulating Wnt signalling in th...

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Bibliographic Details
Main Authors: Nicky J. Willis, Elliott D. Bayle, George Papageorgiou, David Steadman, Benjamin N. Atkinson, William Mahy, Paul V. Fish
Format: Article
Language:English
Published: Beilstein-Institut 2019-11-01
Series:Beilstein Journal of Organic Chemistry
Subjects:
brain penetration
1-chloro-1,2-benziodoxol-3-one
electrophilic chlorination
lp-922056
notum inhibitor
Online Access:https://doi.org/10.3762/bjoc.15.271

Internet

https://doi.org/10.3762/bjoc.15.271

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