3-methoxy-4-(4-methyl-1H-imidazol-1-yl)aniline → (R)-N-(3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl)-6-methyl-8-phenyl-5,6,7,8-tetrahydropyrimido[5,4-f][1,4]oxazepin-2-amine

Participants

Reaction Conditions

Reaction Steps

The aim is optimization. (R)-2-chloro-6-methyl-8-phenyl-5,6,7,8-tetrahydropyrimido[5,4-f][1,4]oxazepine (29 mg, 0.11 mmol), 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)aniline (21.38 mg, 0.11 mmol), Sodium tert-butoxide (15.16 mg, 0.16 mmol), rac-2,2'-Bis(diphenylphosphino)-1,1'-binaphthyl (9.17 mg, 0.01 mmol) and Tris(dibenzylideneacetone)dipalladium(0) (6.74 mg, 7.36 µmol) were added to a microwave vial then toluene (1 mL) was added. The reaction mixture was flushed with nitrogen and the mixture was heated to 120°C for 45 min. Small amount of product was formed. Abandoned.

Provenance & Evidence