Fit-for-purpose synthesis of dual leucine zipper kinase (DLK) inhibitor GNE-834
2020
Xu, Jie | Carrera, Diane E. | Beaudry, Danial | Siu, Kin Wai Michael | Huestis, Malcolm P. | Liu, Wendy | Angelaud, Rémy | Gosselin, Francis
A practical fit-for-purpose synthesis of dual leucine zipper kinase (DLK) inhibitor GNE-834 (1) was developed. The key CC bond was constructed via a Suzuki–Miyaura cross-coupling of iodopyrazole 2 and pyridine boronic ester 3 to afford ketone 12. Subsequent selective reductive amination of ketone 12 with morpholine followed by a resolution via tosylate salt formation provided GNE-834 (1) in 39% overall yield from iodide 2 with 98.9 A% HPLC purity.
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