(R)-吡咯烷-2-乙酸盐酸盐

反应条件: temp:25.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: A solution of (R)-2-carboxymethyl-pyrrolidine-1-carboxylic acid tert-butyl ester in 2 N hydrogen chloride in dioxane (250 mg, 1.1 mmol) in 4 N hydrogen chloride in dioxane (2 ml, 8 mmol) was stirred for 2 h at 25° C. and evaporated to dryness and redissolved in ethanol. After addition of a few drops of 12 M aqueous hydrochloric acid the mixture was stirred at 25° C. overnight. Solvents were evaporated to give 200 mg (95%) of (R)-pyrrolidin-2-yl-acetic acid ethyl ester hydrochloride (25 mg, 55%). evaporated to dryness redissolved in ethanol After addition of a few drops of 12 M aqueous hydrochloric acid the mixture Solvents were evaporated

反应条件: temp:25.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: A solution of (R)-2-carboxymethyl-pyrrolidine-1-carboxylic acid tert-butyl ester in 2 N hydrogen chloride in dioxane (250 mg, 1.1 mmol) in 4 N hydrogen chloride in dioxane (2 ml, 8 mmol) was stirred for 2 h at 25° C. and evaporated to dryness and redissolved in ethanol. After addition of a few drops of 12 M aqueous hydrochloric acid the mixture was stirred at 25° C. overnight. Solvents were evaporated to give 200 mg (95%) of (R)-pyrrolidin-2-yl-acetic acid ethyl ester hydrochloride (25 mg, 55%). evaporated to dryness redissolved in ethanol After addition of a few drops of 12 M aqueous hydrochloric acid the mixture Solvents were evaporated

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

实验步骤: Experimental condition analogous to Example 22 were used with 2-(R)-[(2-methyl-3-phenyl-allylamino)-methyl]-pyrrolidine-1-carboxylic acid tert-butyl ester (prepared according to the scheme 13) were used with 2-(R)-carboxymethyl-pyrrolidine-1-carboxylic acid tert-butyl ester) 0.5 g (1.51 mmol), 3,4,5-trimethoxy benzoic acid 0.38 g (1.8 mmol), triethylamine 0.1 ml, 1-(dimethylaminopropyl)-3-ethylcarbodiimide 0.43 g (2.2 mmol), and 1-hydroxybenzotriazole 0.2 g (1.5 mmol) in 10 ml DCM. The reaction yielded 0.46 g of 2-(R){[2-methyl-3-phenyl-allyl)-3,4,5-trimethoxy-benzoyl)-amino]-methyl}-pyrrolidine-1-carboxylic acid tert-butyl ester. After BOC deprotection analogous to the Example 13, the compound was transformed to the HCl salt, 0.35 g of a white solid was obtained. Yield: 50% prepared

反应条件: temp:25.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: A solution of (R)-2-carboxymethyl-pyrrolidine-1-carboxylic acid tert-butyl ester in 2 N hydrogen chloride in dioxane (250 mg, 1.1 mmol) in 4 N hydrogen chloride in dioxane (2 ml, 8 mmol) was stirred for 2 h at 25° C. and evaporated to dryness and redissolved in ethanol. After addition of a few drops of 12 M aqueous hydrochloric acid the mixture was stirred at 25° C. overnight. Solvents were evaporated to give 200 mg (95%) of (R)-pyrrolidin-2-yl-acetic acid ethyl ester hydrochloride (25 mg, 55%). evaporated to dryness redissolved in ethanol After addition of a few drops of 12 M aqueous hydrochloric acid the mixture Solvents were evaporated