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The title was changed to "Implementation of micelle-enabled C(sp2)–C(sp3) cross-electrophile coupling in pharmaceutical synthesis" during revision

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

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