(2-aminophenyl)-pyrrolidin-1-ylmethanone

反応条件: temp:0.00; pressure:0.00; stir:

反応条件: temp:0.00; pressure:0.00; stir:

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

実験手順: 17.5 g isatoic anhydride and 2.66 g 4-dimethylaminopyridine are combined in 500 ml tetrahydrofuran. 9.32 g of pyrrolidine is added and the mixture is heated at reflux overnight. The mixture is concentrated in vacuo, the residue taken into ethyl acetate and the organic solution washed with citric acid solution, water and brine and dried over magnesium sulfate. The solution is filtered, evaporated and the residue triturated in ether/hexane (1:5) to give N-(2-aminobenzoyl)pyrrolidine, m.p. 79°-81° C. the mixture is heated at reflux overnight The mixture is concentrated in vacuo the organic solution washed with citric acid solution, water and brine dried over magnesium sulfate The solution is filtered evaporated the residue triturated in ether/hexane (1:5)

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

実験手順: The title product was prepared according to the procedure for Example 102 using diethyl (4-{[4-chloro-5-(trifluoromethyl)pyrimidin-2-yl]amino}-3-methoxybenzyl)phosphonate and the commercially available 2-(pyrrolidin-1-ylcarbonyl)aniline.MS (ES+): m/z 608.35 (100) [MH+]; HPLC: tR=1.07 min (UPLC, purity).

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

実験手順: The title product was prepared according to the procedure for Example 102 using diethyl (4-{[4-chloro-5-(trifluoromethyl)pyrimidin-2-yl]amino}-3-methoxybenzyl)phosphonate and the commercially available 2-(pyrrolidin-1-ylcarbonyl)aniline.MS (ES+): m/z 608.35 (100) [MH+]; HPLC: tR=1.07 min (UPLC, purity).

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

実験手順: The title product was prepared according to the procedure for Example 102 using diethyl (4-{[4-chloro-5-(trifluoromethyl)pyrimidin-2-yl]amino}benzyl)phosphonate and the commercially available 2-(pyrrolidin-1-ylcarbonyl)aniline. MS (ES+): m/z 578.34 (100) [MH+]; HPLC: tR=1.02 min (UPLC, purity).

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

実験手順: 17.5 g isatoic anhydride and 2.66 g 4-dimethylaminopyridine are combined in 500 ml tetrahydrofuran. 9.32 g of pyrrolidine is added and the mixture is heated at reflux overnight. The mixture is concentrated in vacuo, the residue taken into ethyl acetate and the organic solution washed with citric acid solution, water and brine and dried over magnesium sulfate. The solution is filtered, evaporated and the residue triturated in ether/hexane (1:5) to give N-(2-aminobenzoyl)pyrrolidine, m.p. 79°-81° C. the mixture is heated at reflux overnight The mixture is concentrated in vacuo the organic solution washed with citric acid solution, water and brine dried over magnesium sulfate The solution is filtered evaporated the residue triturated in ether/hexane (1:5)

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

実験手順: 17.5 g isatoic anhydride and 2.66 g 4-dimethylaminopyridine are combined in 500 ml tetrahydrofuran. 9.32 g of pyrrolidine is added and the mixture is heated at reflux overnight. The mixture is concentrated in vacuo, the residue taken into ethyl acetate and the organic solution washed with citric acid solution, water and brine and dried over magnesium sulfate. The solution is filtered, evaporated and the residue triturated in ether/hexane (1:5) to give N-(2-aminobenzoyl)pyrrolidine, m.p. 79°-81° C. the mixture is heated at reflux overnight The mixture is concentrated in vacuo the organic solution washed with citric acid solution, water and brine dried over magnesium sulfate The solution is filtered evaporated the residue triturated in ether/hexane (1:5)

反応条件: temp:0.00; pressure:0.00; stir:

反応条件: temp:0.00; pressure:0.00; stir:

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

実験手順: The title product was prepared according to the procedure for Example 102 using diethyl(4-{[4-chloro-5-(trifluoromethyl)pyrimidin-2-yl]amino}-3-methoxybenzyl)phosphonate and the commercially available 2-(pyrrolidin-1-ylcarbonyl)aniline. MS (ES+): m/z 608.35 (100) [MH+]; HPLC: tR=1.07 min (UPLC, purity).

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

実験手順: The title product was prepared according to the procedure for Example 102 using diethyl (4-{[4-chloro-5-(trifluoromethyl)pyrimidin-2-yl]amino}-3-methoxybenzyl)phosphonate and the commercially available 2-(pyrrolidin-1-ylcarbonyl)aniline.MS (ES+): m/z 608.35 (100) [MH+]; HPLC: tR=1.07 min (UPLC, purity).