Improved synthesis of sterically encumbered heteroaromatic biaryls from aromatic beta-keto esters

Brandon R. Rosen,Ehesan Ul Sharif,Dillon H. Miles, Nicholas S. Chan,Manmohan R. Leleti,Jay P. Powers

Tetrahedron Letters（2020）

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摘要

•Aryl substituted 2-aminopyrimidines are important in drug discovery.•AB928 is a potent A2a/A2bR antagonist undergoing clinical trials in cancer.•Trifluoroethanol promotes reaction between hindered β-keto esters with guanidine.

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关键词

Heterocycle,Aminopyrimidine,Guanidine condensation,AB928

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