N-[(2-bromophenyl)methyl]-1-cyclopropylmethanamine

反応条件: temp:120.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: 114 mg of (2-bromobenzyl)cyclopropylmethylamine, 100 mg of potassium carbonate, 7 μl of water and 29 mg of [1,1′-bis(diphenylphosphino)ferrocene]-palladium(II) dichloride are added to a solution of 150 mg of [2-amino-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)quinazolin-4-yl]-(1,3-dihydroisoindol-2-yl)methanone in 5 ml of ethanol under argon. The mixture is heated at 120° C. for 30 min; the hot mixture is filtered through kieselguhr, the filtrate is evaporated and purified by chromatography (reversed phase HPLC). the hot mixture is filtered through kieselguhr the filtrate is evaporated purified by chromatography (reversed phase HPLC)

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: 53 mg of sodium hydride in 3 ml of tetrahydrofuran are added to 300 mg of (2-bromobenzyl)cyclopropylamine in 2 ml of tetrahydrofuran with ice-cooling. 207 μl of iodomethane are subsequently added, and the mixture is heated at 600 for 1 h. The mixture is allowed to cool and poured onto 20 g of ice and 5 ml of 1N hydrochloric acid, washed 4 times with 10 ml of ethyl acetate each time, and the combined organic phases are dried over sodium sulfate. After filtration, the filtrate is evaporated to dryness. cooling the mixture is heated at 600 for 1 h to cool washed 4 times with 10 ml of ethyl acetate each time the combined organic phases are dried over sodium sulfate After filtration the filtrate is evaporated to dryness