Implementation of micelle-enabled C(sp2)–C(sp3) cross-electrophile coupling in pharmaceutical synthesis

Author:

Wu Bin1,Ye Ning1,Zhao Kangming1ORCID,Shi Min1,Liao Jiayu1,Zhang Jing1,Chen Wei1,Li Xianzhong1,Han Yufeng1,Cortes-Clerget Margery2,Regnier Morgan Louis2,Parmentier Michael2ORCID,Mathes Christian2,Rampf Florian2,Gallou Fabrice2ORCID

Affiliation:

1. Chemical & Analytical Development, Suzhou Novartis Technical Development Co., Ltd, Changshu, Jiangsu 215537, China

2. Chemical & Analytical Development, Novartis Pharma AG, 4056 Basel, Switzerland

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, leading to a key intermediate of one of our development compounds.

Funder

Novartis

Publisher

Royal Society of Chemistry (RSC)

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