Jiang, Hao, Rufle, Dominik, Parmentier, Michael, Gallou, Fabrice and Wu, Bin (2024) 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. Helvetica Chimica Acta, 107 (8). e202400094-e202400094. ISSN 0018-019X1522-2675

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.

Item Type:	Article
Date Deposited:	27 Aug 2024 00:46
Last Modified:	27 Aug 2024 00:46
URI:	https://oak.novartis.com/id/eprint/53600