4-(3-fluoropiperidin-4-yl)morpholine

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

実験手順: 4-(3-Fluoro-piperidin-4-yl)-morpholine (0.085 g, 0.45 mmol), 2-(3-Bromo-phenyl)-1-methyl-1H-benzoimidazole (described in method N, step a, b) (0.10 g, 0.35 mmol), and cesium carbonate (10.50 g, 32.2 mmol) were placed into a dry sealed 7 mL vial under nitrogen and dry toluene (0.4 mL) was added. At the same time Palladium acetate (0.016 g, 0.07 mmol), and BINAP (0.065 g, 0.10 mmol) were placed into another dry sealed 7 mL vial under nitrogen and diluted with dry toluene (0.8 mL) After about 20 minutes the resulting suspension was added to the vial containing the starting materials. was added sealed 7 mL vial under nitrogen was added to the vial containing the starting materials

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

実験手順: 2.0 N HCl in Et2O (15 mL) was added to a solution of 3-Fluoro-4-morpholin-4-yl-piperidine-1-carboxylic acid tert-butyl ester (1.28 g, 4.44 mmol) in DCM (2 mL) and the resulting suspension was stirred at room temperature 4 days. The precipitate was filtered off and tritured with Et2O (2×5 mL) Na2CO3 saturated solution (10 mL) was added and the resulting solution was concentrated under reduced pressure. EtOH (15 mL) was added and precipitate was filtered off. The precipitate was filtered off was added the resulting solution was concentrated under reduced pressure EtOH (15 mL) was added precipitate was filtered off