1-Pyrrolidineethanamine → HCID 68777550, compound

Participants

Reaction Steps

Benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate (145 mg, 0.33 mmol) and 1-(2-aminoethyl)pyrrolidine (60 μL, 0.49 mmol) were added to a solution of Example 292 (70 mg, 0.16 mmol) in DCM (10 mL) and the reaction mixture was stirred at room temperature for 18 h. A further portion of 1-(2-aminoethyl)-pyrrolidine (60 μL, 0.49 mmol) was added and stirring was continued for 72 h. The solvent was removed in vacuo and the residue was purified by preparative HPLC (pH 2.5) to give the title compound (16 mg, 19%) as an off-white solid. δH (CDCl3) 9.26 (1H, s), 8.43 (1H, br s), 7.74-7.69 (1H, m), 7.65-7.59 (1H, m), 7.45 (1H, t, J 7.7 Hz), 7.23-7.16 (1H, m), 3.78-3.64 (6H, m), 3.11-2.92 (10H, m), 2.49 (2H, s), 2.45 (2H, s), 2.07-1.96 (4H, m), 1.05 (6H, s). LCMS (ES+) 525.3 (M+H)+.

Provenance & Evidence