Abstract
The structure of primary alkylated arenes plays an important role in the molecular action of drugs and natural products. The nickel/spiro-bidentate-pyox catalysed cross-electrophile coupling of aryl bromides and primary alkyl bromides was developed for the formation of the Csp2–Csp3 bond, which provided an efficient method for the synthesis of primary alkylated arenes. The reactions could tolerate functional groups such as ester, aldehyde, ketone, ether, benzyl, and imide.
Highlights
Numerous attractive synthesis approaches to primary alkylated arenes have been developed, primarily based on the transition metal-catalysed addition of nucleophiles to electrophiles.[1]
The direct use of electrophiles is convenient because electrophiles are more accessible and easier to use than nucleophiles in the coupling reactions
The cross electrophile coupling reactions catalysed by nickel metal catalysts can provide effective methods for the construction of new C–C bonds in drugs and natural products.2b,3 Previous studies have established that 5HT2A agonists have been implicated in cardiovascular function[4] (Scheme 1)
Summary
Numerous attractive synthesis approaches to primary alkylated arenes have been developed, primarily based on the transition metal-catalysed addition of nucleophiles to electrophiles.[1]. The cross electrophile coupling reactions catalysed by nickel metal catalysts can provide effective methods for the construction of new C–C bonds in drugs and natural products.2b,3 Previous studies have established that 5HT2A agonists have been implicated in cardiovascular function[4] (Scheme 1). Charboneau et al.[8] used a dual metal catalytic system for cross-electrophile coupling reactions between aryl halides and alkyl halides (Scheme 2a).
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