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Micelle Enabled Buchwald‐Hartwig Amination in Water with the Bening by Design Surfactant TPGS‐750‐M for the Synthesis of the JAK Inhibitor 4‐((2‐Chlorophenyl)amino)‐6‐((6‐methylpyridin‐2‐yl)amino)nicotinamide

Authors :
Jiang, Hao
Wu, Bin
Rufle, Dominik
Wang, Liping
Shi, Min
Parmentier, Michael
Gallou, Fabrice
Source :
Helvetica Chimica Acta. Sep2024, Vol. 107 Issue 9, p1-9. 9p.
Publication Year :
2024

Abstract

An efficient and scalable Buchwald‐Hartwig amination towards the synthesis of the API candidate 4‐((2‐Chlorophenyl)amino)‐6‐((6‐methylpyridin‐2‐yl)amino)nicotinamide as a JAK inhibitor was described. The process was developed using water and a water‐miscible co‐solvent. It was facilitated by the benign by design surfactant TPGS‐750‐M, that promoted the robust and reliable preparation of our target compound in high yields, with improved reaction profile and via an operationally simple protocol. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
0018019X
Volume :
107
Issue :
9
Database :
Academic Search Index
Journal :
Helvetica Chimica Acta
Publication Type :
Academic Journal
Accession number :
180681507
Full Text :
https://doi.org/10.1002/hlca.202400094