Development of a Scalable Negishi Cross-Coupling Process for the Preparation of 2-Chloro-5-(1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazol-5-yl)aniline

Candice L. Joe,Bahar Inankur,James Chadwick,Sha Lou,Jeffrey Nye,Neil A. Strotman,Albert J. DelMonte

Organic Process Research & Development（2020）

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摘要

A scalable synthesis of 2-chloro-5-(1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazol-5-yl)aniline (1), a key intermediate in the synthesis of an immuno-oncology asset, is described. A Negishi cross-coupling...

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关键词

Zinc,Negishi,Pd-catalyzed,metals remediation,pyrazole,hexyllithium

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