In this section, you can access to the latest technical information related to the FUTURE project topic.

Palladium?catalyzed ?on?water? tandem cyclization reactions for the synthesis of biologically important 4?arylquinazolines

The privileged quinazoline scaffold is prevalent in pharmaceutically relevant molecules that show diverse biological activities. Herein we report an efficient palladium?catalyzed ?on?water? tandem cyclization reactions from commercially available arylboronic acids and benzonitriles that enable rapid access to the 4?arylquinazoline scaffolds in good to excellent yields (45 examples, up to 98% yield). This protocol has shown good functional group tolerance and broad substrate scope. The reaction was also performed on a gram scale and successfully applied to the synthesis of highly potent and selective PI3K? inhibitor N11, showing the practicability and synthetic utility of the protocol. In this reaction, the quinazoline scaffold is efficiently constructed with one C?C bond and one C?N bond formed simultaneously. Collectively, the protocol could serve as an alternative strategy to synthesize biologically important quinazoline scaffolds.

» Author: Shuo Yuan, Bin Yu, Hong-Min Liu

» Reference: doi:10.1002/chem.201903464

» Publication Date: 21/08/2019

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