Fit-for-purpose synthesis of dual leucine zipper kinase (DLK) inhibitor GNE-834

Jie Xu,Diane E. Carrera,Danial Beaudry,Michael Siu,Malcolm P. Huestis,Wendy Liu,Rémy Angelaud,Francis Gosselin

TETRAHEDRON LETTERS（2020）

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摘要

A practical fit-for-purpose synthesis of dual leucine zipper kinase (DLK) inhibitor GNE-834 (1) was developed. The key C-C 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. (C) 2020 Elsevier Ltd. All rights reserved.

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关键词

Suzuki coupling,Reductive amination,Resolution,DLK inhibitor,ALS

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