2-Fluoro-4-(methylsulphonyl)aniline → tert-butyl 4-(4-{[2-fluoro-4-(methylsulfonyl)phenyl]amino}-5H-pyrrolo[3,2-d]pyrimidin-7-yl)piperidine-1-carboxylic acid

Participants

Reaction Steps

tert-Butyl 4-(4-chloro-5H-pyrrolo[3,2-d]pyrimidin-7-yl)piperidine-1-carboxylate (54.8 mg, 0.163 mmol) was dissolved in 1,4-dioxane (0.5 mL), 2-fluoro-4-methylsulfonylaniline (32.0 mg, 0.169 mmol), tert-butoxysodium (15.9 mg, 0.109 mmol) and bis(tri-tert-butyl-phosphine)palladium (0) (5.8 mg, 0.011 mmol) were added, and the mixture was irradiated with microwave in a sealed tube at 130° C. for 3 hours. The reaction liquid was filtered, the filtrate was concentrated under a reduced pressure, and the obtained residue was purified by using silica gel chromatography (ethyl acetate:hexane=3:1) to give the titled compound (3.6 mg, 6.5%) as a white amorphous.

Provenance & Evidence