Supporting Information
(1) experimental procedures and characterisation data for 3–10 and 1; (2) mouse PK data which includes: study design summary; plasma concentrations; brain concentrations; (3) Notum IC50 (nM), MLM Cli (μL/min/mg protein) and MDCK-MDR1 AB/BA Papp (× 10−6 cm/s) data for 17a–r.
To view the NMR spectra, use the file within the pdata folder of Supporting Information File 3.
| Supporting Information File 1: Experimental section, mouse pharmacokinetics and profiles of amides. | ||
| Format: PDF | Size: 905.8 KB | Download |
| Supporting Information File 2: Profiles of amides. | ||
| Format: CSV | Size: 1.3 KB | Download |
| Supporting Information File 3: Raw NMR data files for compound LP-922056. | ||
| Format: ZIP | Size: 2.4 MB | Download |
Cite the Following Article
An improved, scalable synthesis of Notum inhibitor LP-922056 using 1-chloro-1,2-benziodoxol-3-one as a superior electrophilic chlorinating agent
Nicky J. Willis, Elliott D. Bayle, George Papageorgiou, David Steadman, Benjamin N. Atkinson, William Mahy and Paul V. Fish
Beilstein J. Org. Chem. 2019, 15, 2790–2797.
https://doi.org/10.3762/bjoc.15.271
How to Cite
Willis, N. J.; Bayle, E. D.; Papageorgiou, G.; Steadman, D.; Atkinson, B. N.; Mahy, W.; Fish, P. V. Beilstein J. Org. Chem. 2019, 15, 2790–2797. doi:10.3762/bjoc.15.271
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