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■ A Novel Synthesis of a 1,3-Disubstituted 1,3-Dihydro-2H-imidazo[4,5-b]pyridin-2-one. Application to GW808990 a CRF1 Receptor Antagonist

Jerome F. Hayes* and Matthew E. Popkin

*GlaxoSmithKline Research & Development Ltd., Old Powder Mills, Old Powdermill Lane, Leigh, Nr Tonbridge, Kent, TN11 9AN, U.K.

Abstract

A novel synthesis of a 1,3-disubstituted 1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-one has been achieved by condensation of iminohydantoin 3 with t-butyl acetoacetate in diglyme at 160 °C. Hydrogenation of the product in the presence of 4-heptanone followed by a Buchwald-Hartwig amination afforded GW808990, a CRF1 receptor antagonist.