Wu, Bin, Ye, Ning, Zhang, Jing, Chen, Wei, Li, Xianzhong, Han, Yufeng, Parmentier, Michael, Mathes, Christian, Rampf, Florian and Gallou, Fabrice (2024) The title was changed to "Implementation of micelle-enabled C(sp2)–C(sp3) cross-electrophile coupling in pharmaceutical synthesis" during revision. Chemical communications, NA (NA). NA. ISSN 1364-548X; 1359-7345

Abstract

A sustainable C(sp2)-C(sp3) cross- electrophile coupling was developed between readily available 5-bromophthalide and 1-benzyl-4-iodopiperidine under micellar conditions in water, leading to the key intermediate of one of our development compounds. Copper was found to play a crucial role as co-catalyst in this due catalysis system. The chemistry and process were successfully demonstrated in kilo scale to deliver sufficient drug substance to the clinical campaigns.

Item Type:	Article
Date Deposited:	17 Feb 2024 00:46
Last Modified:	17 Feb 2024 00:46
URI:	https://oak.novartis.com/id/eprint/52096