Parmentier, Michael, Gallou, Fabrice, Wickendick, Regina, Wagner, Mona, Langlois, Audrey and Baenziger, Markus (2020) A general kilogram scale protocol for Suzuki-Miyaura cross-coupling in water with TPGS-750-M surfactant. Organic Process Research & Development. ISSN 1083-61601520-586X

Abstract

The development of a kilogram scale protocol for a Suzuki–Miyaura cross-coupling step toward the synthesis of the drug candidate LSZ102 is described. Particularly, the use of the surfactant TPGS-750-M in water as a medium for the transformation and its impact on the selectivity and quality are reported. Minimization of typical impurities generated during the cross-coupling (e.g., dehalogenation) has been in focus during our study. The environmental and cost impacts using such a process are also discussed.

Item Type:	Article
Keywords:	TPGS-750-M, surfactant, micelles, palladium-catalyzed reactions; Suzuki-Miyaura cross-coupling, LSZ102
Date Deposited:	27 Aug 2020 00:45
Last Modified:	27 Aug 2020 00:45
URI:	https://oak.novartis.com/id/eprint/42792