2-(六甲撑亚胺)乙醇

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: By treating 17.31 g of methyl 2-(7-trifluoromethyl-4-quinolyl)aminobenzoate (II, R=CF3, R"=CH3), 10.5 g of 1-(2-hydroxyethyl)homopiperidine in 130 ml of toluene and in the presence of sodium as described in Example 1, 20.6 g of a crude material are isolated. The recrystallization in diisopropyl ether enables to isolate 13.7 g (yield: 60%) of a whitish solid with m.p. 72°-75° C. and elemental analysis C, H, N, F correct. are isolated The recrystallization in diisopropyl ether

反应条件: temp:0.00; pressure:0.00; stir:

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: By treating 17.31 g of methyl 2-(7-trifluoromethyl-4-quinolyl)aminobenzoate (II, R=CF3, R"=CH3), 10.5 g of 1-(2-hydroxyethyl)homopiperidine in 130 ml of toluene and in the presence of sodium as described in Example 1, 20.6 g of a crude material are isolated. The recrystallization in diisopropyl ether enables to isolate 13.7 g (yield: 60%) of a whitish solid with m.p. 72°-75° C. and elemental analysis C, H, N, F correct. are isolated The recrystallization in diisopropyl ether

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: By treating 17.31 g of methyl 2-(7-trifluoromethyl-4-quinolyl)aminobenzoate (II, R=CF3, R"=CH3), 10.5 g of 1-(2-hydroxyethyl)homopiperidine in 130 ml of toluene and in the presence of sodium as described in Example 1, 20.6 g of a crude material are isolated. The recrystallization in diisopropyl ether enables to isolate 13.7 g (yield: 60%) of a whitish solid with m.p. 72°-75° C. and elemental analysis C, H, N, F correct. are isolated The recrystallization in diisopropyl ether

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: To a solution of 2-azepan-1-ylethanol (5.0 g) in N,N-dimethylformamide (100 ml) was added 60% sodium hydride (1.5 g) under a nitrogen atmosphere, the solution was stirred for 1 hour at room temperature, 2,5-dibromopyridine (7.5 g) was then added thereto followed by stirring for 4.5 hours at room temperature. Water was added thereto followed by stirring, the solution was extracted with ethyl acetate, then sequentially washed with water and brine, dried over anhydrous magnesium sulfate, and then the solvent was evaporated in vacuo. The residue was purified by NH silica gel column chromatography (hexane-ethyl acetate system) to provide the title compound (9.1 g). by stirring for 4.5 hours at room temperature by stirring the solution was extracted with ethyl acetate sequentially washed with water and brine dried over anhydrous magnesium sulfate the solvent was evaporated in vacuo The residue was purified by NH silica gel column chromatography (hexane-ethyl acetate system)

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: To a solution of 2-azepan-1-ylethanol (5.0 g) in N,N-dimethylformamide (100 ml) was added 60% sodium hydride (1.5 g) under a nitrogen atmosphere, the solution was stirred for 1 hour at room temperature, 2,5-dibromopyridine (7.5 g) was then added thereto followed by stirring for 4.5 hours at room temperature. Water was added thereto followed by stirring, the solution was extracted with ethyl acetate, then sequentially washed with water and brine, dried over anhydrous magnesium sulfate, and then the solvent was evaporated in vacuo. The residue was purified by NH silica gel column chromatography (hexane-ethyl acetate system) to provide the title compound (9.1 g). by stirring for 4.5 hours at room temperature by stirring the solution was extracted with ethyl acetate sequentially washed with water and brine dried over anhydrous magnesium sulfate the solvent was evaporated in vacuo The residue was purified by NH silica gel column chromatography (hexane-ethyl acetate system)

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: To a solution of 2-azepan-1-ylethanol (5.0 g) in N,N-dimethylformamide (100 ml) was added 60% sodium hydride (1.5 g) under a nitrogen atmosphere, the solution was stirred for 1 hour at room temperature, 2,5-dibromopyridine (7.5 g) was then added thereto followed by stirring for 4.5 hours at room temperature. Water was added thereto followed by stirring, the solution was extracted with ethyl acetate, then sequentially washed with water and brine, dried over anhydrous magnesium sulfate, and then the solvent was evaporated in vacuo. The residue was purified by NH silica gel column chromatography (hexane-ethyl acetate system) to provide the title compound (9.1 g). by stirring for 4.5 hours at room temperature by stirring the solution was extracted with ethyl acetate sequentially washed with water and brine dried over anhydrous magnesium sulfate the solvent was evaporated in vacuo The residue was purified by NH silica gel column chromatography (hexane-ethyl acetate system)

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: To a solution of 2-azepan-1-ylethanol (5.0 g) in N,N-dimethylformamide (100 ml) was added 60% sodium hydride (1.5 g) under a nitrogen atmosphere, the solution was stirred for 1 hour at room temperature, 2,5-dibromopyridine (7.5 g) was then added thereto followed by stirring for 4.5 hours at room temperature. Water was added thereto followed by stirring, the solution was extracted with ethyl acetate, then sequentially washed with water and brine, dried over anhydrous magnesium sulfate, and then the solvent was evaporated in vacuo. The residue was purified by NH silica gel column chromatography (hexane-ethyl acetate system) to provide the title compound (9.1 g). by stirring for 4.5 hours at room temperature by stirring the solution was extracted with ethyl acetate sequentially washed with water and brine dried over anhydrous magnesium sulfate the solvent was evaporated in vacuo The residue was purified by NH silica gel column chromatography (hexane-ethyl acetate system)