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Step 1 Methyl 1-benzyl-5-oxo-3-pyrrolidinecarboxylate (50 g, 0.21 mol) was stirred in a solution of ammonia in methanol (7 M, 400 mL, 2.8 mol). After 2 days, the solution was concentrated with heating (50 C.) to about 300 mL at which point all solids remained dissolved. The reaction was then allowed to cool down and the resulting solid was filtered, washed with ether and dried to give 1-benzyl-5-oxo-pyrrolidine-3-carboxylic acid amide as colorless crystals (40 g).
4.2 Step 2
Step 2 1-Benzyl-5-oxo-pyrrolidine-3-carboxylic acid amide (22 g, 0.1 mol) was added portionwise to a stirred solution of lithium aluminum hydride (9.5 g, 0.25 mol, 2.5 equiv.) in dry tetrahydrofuran (600 mL). After the initial effervescence had subsided, the reaction mixture was heated at reflux at room temperature for 24 h, at which time analysis of the reaction mixture by LCMS showed there was no starting material. The reaction mixture was quenched by dropwise addition of saturated sodium sulphate solution with stirring until no further effervescence was observed. The suspension was filtered through a celite plug, eluding with diethyl ether (200 mL). The solvent was remove to afford 3-(RS)-aminomethyl-1-benzylpyrrolidine as an oil (14.7 g) which was used directly without further purification.
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