Cesium carbonate → N-[2-Chloro-4-(trifluoromethyl)phenyl]-1-methyl-7-(4-morpholinylcarbonyl)-1H-pyrrolo[3,2-c]pyridin-4-amine hydrochloride

Participants

Reaction Conditions

Reaction Steps

A mixture of 4-chloro-1-methyl-7-(4-morpholinylcarbonyl)-1H-pyrrolo[3,2-c]pyridine (100 mg), 2-chloro-4-trifluoromethylaniline (80 mg), cesium carbonate (168 mg), tris(dibenzylideneacetone)dipalladium (0) (3.4 mg) and 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene (2.3 mg) in 1,4-dioxan (2 ml) was heated to 100° C. under nitrogen for 2 h. Added tris(dibenzylideneacetone)dipalladium (0) (10 mg) and 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene (7 mg) and continued heating at 100° C. under nitrogen over night. The reaction mixture was diluted with dichloromethane and washed with water then dried (MgSO4), filtered and evaporated. Purification and salt formation was as described in Example 101 to afford the title compound as a white solid (64 mg).

Provenance & Evidence