A NOVEL SYNTHESIS OF A 1,3-DISUBSTITUTED 1,3-DIHYDRO-2H-IMIDAZO4,5-bPYRIDIN-2-ONE. APPLICATION TO GW808990 A CRF1 RECEPTOR ANTAGONIST

摘要

A novel synthesis of a 1,3-disubstituted 1,3-dihydro-2H-imidazo-4,5-bpyridin-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 animation afforded GW808990, a CRF1 receptor antagonist.