2-(methylamino)ethanesulfonic acid

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:

反応条件: temp:50.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: 130 mg of 3-[3-(4-fluorophenyl)-3-hydroxypropyl]-1-[4-(4-fluorobutoxy)phenyl]-4-(4-methoxyphenyl)azetidin-2-one (7) were dissolved in 6 ml of absolute methanol. 120 mg of N-methyltaurine in 2 ml of water and 60 mg of potassium carbonate were then added. The mixture was stirred at 50° C. for 24 h. The reaction mixture was concentrated using a rotary evaporator and the residue was purified by preparative chromatography. Freeze-drying gave the product (50 mg) as an oil. The reaction mixture was concentrated a rotary evaporator the residue was purified by preparative chromatography Freeze-drying

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: To a stirred solution of 2-methylaminoethane-1-sulfonic acid, sodium salt (16.1 g, 100 mmol), in aq. sodium hydroxide (1M, 100 mL, 100 mmol) at 0° C., benzyl chloroformate (16 mL, 112 mmol) was added over a period of 15 minutes. The resulting mixture was stirred at room temperature for 2 hours and extracted with hexane. The aqueous solution was freeze dried to provide 2-[[(benzyloxy)carbonyl](methyl)amino]-ethane-1-sulfonic acid, sodium salt. extracted with hexane dried

反応条件: temp:50.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: 130 mg of 3-[3-(4-fluorophenyl)-3-hydroxypropyl]-1-[4-(4-fluorobutoxy)phenyl]-4-(4-methoxyphenyl)azetidin-2-one (7) were dissolved in 6 ml of absolute methanol. 120 mg of N-methyltaurine in 2 ml of water and 60 mg of potassium carbonate were then added. The mixture was stirred at 50° C. for 24 h. The reaction mixture was concentrated using a rotary evaporator and the residue was purified by preparative chromatography. Freeze-drying gave the product (50 mg) as an oil. The reaction mixture was concentrated a rotary evaporator the residue was purified by preparative chromatography Freeze-drying

反応条件: temp:50.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: 130 mg of 3-[3-(4-fluorophenyl)-3-hydroxypropyl]-1-[4-(4-fluorobutoxy)phenyl]-4-(4-methoxyphenyl)azetidin-2-one (7) were dissolved in 6 ml of absolute methanol. 120 mg of N-methyltaurine in 2 ml of water and 60 mg of potassium carbonate were then added. The mixture was stirred at 50° C. for 24 h. The reaction mixture was concentrated using a rotary evaporator and the residue was purified by preparative chromatography. Freeze-drying gave the product (50 mg) as an oil. The reaction mixture was concentrated a rotary evaporator the residue was purified by preparative chromatography Freeze-drying

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:50.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: 130 mg of 3-[3-(4-fluorophenyl)-3-hydroxypropyl]-1-[4-(4-fluorobutoxy)phenyl]-4-(4-methoxyphenyl)azetidin-2-one (7) were dissolved in 6 ml of absolute methanol. 120 mg of N-methyltaurine in 2 ml of water and 60 mg of potassium carbonate were then added. The mixture was stirred at 50° C. for 24 h. The reaction mixture was concentrated using a rotary evaporator and the residue was purified by preparative chromatography. Freeze-drying gave the product (50 mg) as an oil. The reaction mixture was concentrated a rotary evaporator the residue was purified by preparative chromatography Freeze-drying

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

実験手順: Among them, particularly preferable are ammonia, ethylamine, taurine, N-methyltaurine, methylamine, n-propylamine, monoethanolamine, β-alanine, 2-chloroethylamine, 2-sulfatoethylamine, aniline, aniline-2-, -3- or -4-sulfonic acid, 2-, 3- or 4-carboxyaniline, N-methylaniline, N-ethylaniline, N-ethyl-2-, -3- or -4-chloroaniline, aniline-2,4- or -2,5-disulfonic acid, 2-, 3- or 4-chloroaniline, 2-, 3- or 4-methylaniline, 3- or 4-methylaminobenzenesulfonic acid, and the like.