2-bromo-1-[2-(trifluoromethoxy)phenyl]ethanone

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

実験手順: The title compound was synthesized in analogy to example 7, using 3-oxo-butyric acid methyl ester as compound of formula R, 2-bromo-1-[2-(trifluoromethoxy)phenyl]-ethanone as compound of formula S, (R)-tetrahydrofurfurylamine as R3—(CH2)m—NH2 and trans-2-aminocyclohexanol as R1R2NH, MS (ISP) 467.5 (M+H)+.

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

実験手順: The title compound was synthesized in analogy to example 7, using 3-oxo-butyric acid methyl ester as compound of formula R, 2-bromo-1-[2-(trifluoromethoxy)phenyl]-ethanone as compound of formula S, 1,4-dioxane-2-methanamine as R3—(CH2)m—NH2 and cyclohexylamine as R1R2NH, MS (ISP) 467.5 (M+H)+.

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

実験手順: The title compound was synthesized in analogy to example 7, using 3-oxo-butyric acid methyl ester as compound of formula R, 2-bromo-1-[2-(trifluoromethoxy)phenyl]-ethanone as compound of formula S, 2,2-dimethyl-1,3-dioxolan-4-methylamine as R3—(CH2)m—NH2 and cyclohexylamine as R1R2NH, MS (ISP) 481.5 (M+H)+.

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

実験手順: The title compound was synthesized in analogy to example 7, using 3-oxo-butyric acid methyl ester as compound of formula R, 2-bromo-1-[2-(trifluoromethoxy)phenyl]-ethanone as compound of formula S, (R)-tetrahydrofurfurylamine as R3—(CH2)m—NH2 and cyclohexylamine as R1R2NH, MS (ISP) 451.5 (M+H)+.

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

実験手順: To a solution of 2.6 g of 3-oxo-butyric acid methyl ester in THF (50 ml) and 4.6 ml of a solution of sodium methoxide (5.4 M in methanol) was added over 15 minutes a solution of 6.7 g of 2-bromo-1-[2-(trifluoromethoxy)phenyl]-ethanone in 30 ml of THF. The reaction mixture was allowed to stir at room temperature for 17 hours. The solvent was removed, the residue was diluted in diethyl ether and washed several times with water. The organic phase was dried with sodium sulfate and concentrated in vacuo. The residue was purified by column chromatography (silica gel; heptane/ethyl acetate) to give 5.1 g of the title compound. MS (EI) 319.1 (M+H)+. The solvent was removed the residue was diluted in diethyl ether washed several times with water The organic phase was dried with sodium sulfate concentrated in vacuo The residue was purified by column chromatography (silica gel; heptane/ethyl acetate)

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

実験手順: The title compound was synthesized in analogy to example 7, using 3-oxo-butyric acid methyl ester as compound of formula R, 2-bromo-1-[2-(trifluoromethoxy)phenyl]-ethanone as compound of formula S, (R)-tetrahydrofurfurylamine as R3—(CH2)m—NH2 and trans-2-aminocyclohexanol as R1R2NH, MS (ISP) 467.5 (M+H)+.

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

実験手順: The title compound was synthesized in analogy to example 7, using 3-oxo-butyric acid methyl ester as compound of formula R, 2-bromo-1-[2-(trifluoromethoxy)phenyl]-ethanone as compound of formula S, 1,4-dioxane-2-methanamine as R3—(CH2)m—NH2 and cyclohexylamine as R1R2NH, MS (ISP) 467.5 (M+H)+.

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

実験手順: The title compound was synthesized in analogy to example 7, using 3-oxo-butyric acid methyl ester as compound of formula R, 2-bromo-1-[2-(trifluoromethoxy)phenyl]-ethanone as compound of formula S, 2,2-dimethyl-1,3-dioxolan-4-methylamine as R3—(CH2)m—NH2 and cyclohexylamine as R1R2NH, MS (ISP) 481.5 (M+H)+.

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

実験手順: The title compound was synthesized in analogy to example 7, using 3-oxo-butyric acid methyl ester as compound of formula R, 2-bromo-1-[2-(trifluoromethoxy)phenyl]-ethanone as compound of formula S, (R)-tetrahydrofurfurylamine as R3—(CH2)m—NH2 and cyclohexylamine as R1R2NH, MS (ISP) 451.5 (M+H)+.

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

実験手順: To a solution of 2.6 g of 3-oxo-butyric acid methyl ester in THF (50 ml) and 4.6 ml of a solution of sodium methoxide (5.4 M in methanol) was added over 15 minutes a solution of 6.7 g of 2-bromo-1-[2-(trifluoromethoxy)phenyl]-ethanone in 30 ml of THF. The reaction mixture was allowed to stir at room temperature for 17 hours. The solvent was removed, the residue was diluted in diethyl ether and washed several times with water. The organic phase was dried with sodium sulfate and concentrated in vacuo. The residue was purified by column chromatography (silica gel; heptane/ethyl acetate) to give 5.1 g of the title compound. MS (EI) 319.1 (M+H)+. The solvent was removed the residue was diluted in diethyl ether washed several times with water The organic phase was dried with sodium sulfate concentrated in vacuo The residue was purified by column chromatography (silica gel; heptane/ethyl acetate)

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

実験手順: The title compound was synthesized in analogy to Example 68, using 3-oxo-butyric acid methyl ester as compound of formula R, 2-bromo-1-(2-trifluoromethoxy-phenyl)-ethanone as compound of formula S, 2-aminomethyl-1-cyclohexanol as R3—(CH2)m—NH2 and cyclohexylamine as R1R2NH, MS (ISP) 479.6 (M+H)+.

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

実験手順: The title compound was synthesized in analogy to Example 68, using 3-oxo-butyric acid methyl ester as compound of formula R, 2-bromo-1-(2-trifluoromethoxy-phenyl)-ethanone as compound of formula S, 2-aminomethyl-1-cyclohexanol as R3—(CH2)m—NH2 and cyclohexylamine as R1R2NH, MS (ISP) 479.6 (M+H)+.