4-Methoxy-2-pyrimidinamine → tert-butyl N-[1-[4-(7-oxo-3-phenyl-1H-imidazo[1,2-a]pyrimidin-2-yl)phenyl]cyclobutyl]carbamate

Participants

Reaction Conditions

Reaction Steps

A mixture of crude {1-[4-(2-bromo-2-phenyl-acetyl)-phenyl]-cyclobutyl}-carbamic acid tert-butyl ester [Int-1-A] (1.26 g) and 4-methoxypyrimidin-2-ylamine (0.67 g) in DMF (21 mL) was heated overnight at 90° C. (bath temperature). On cooling the mixture was partitioned between EtOAc and water and the organic phase washed with brine, dried and concentrated to give a mixture of the title compound and Int-2-0. Purification was achieved by preparative HPLC to give the title compound.

Provenance & Evidence