6-chloro-1H-indazol-3-amine

Uses

Starting from 6-chloro-1H-indazol-3-amine, the EDC/HOAt promoted coupling with the (S)-carboxylic acid derivative furnished (S)-1-(3-Amino-6-chloro-1H-indazol-1-yl)-2-methyl-3-phenoxypro-pan-1-one. This synthesis was performed to explore the structure-activity relationships (SAR) by substituting the indazole scaffold at the 6-position with a chlorine atom, facilitating the identification of novel CFTR potentiators.^[1]

References

[1] Liu, F., Kaplan, A. L., Levring, J., Einsiedel, J., Tiedt, S., Distler, K., Omattage, N. S., Kondratov, I. S., Moroz, Y. S., Pietz, H. L., Irwin, J. J., Gmeiner, P., Shoichet, B. K., & Chen, J. (2024). Structure-based discovery of CFTR potentiators and inhibitors. Cell, 42 1. https://doi.org/10.1016/j.cell.2024.04.046