Ammonium formate → HCID 10542998, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of (3S)-3-(N-benzyl)aminomethyl-1-[2-(5-(1,2,4-triazol-4-yl)-1H-indol-3-yl)ethyl]pyrrolidine (Example 7; 0.277 g, 0.639 mmol), ammonium formate (0.218 g, 3.46 mmol) and 10% Pd-C (0.28 g), in anhydrous methanol (20 ml) was stirred at 62° C. for 0.75 h. The mixture was cooled to 25° C. and the catalyst removed filtration through celite. The solvent was removed under vacuum and the residue chromatographed on silica gel eluting with CH2Cl2 /MeOH/NH3 (20:8:1) to give the title compound (0.145 g, 68%), δ (250 MHz, CDCl3) 1.48-1.59 (1H, m, CH of CH2), 2.03-2.14 (1H, m, CH of CH2), 2.29-2.41 (2H, m, 2 of CH), 2.63-3.02 (9H, m, 4 of CH2 and CH), 7.14 (1H, dd, J=2.1 and 8.6 Hz, Ar--H), 7.21 (1H, s, Ar--H), 7.49 (1H, d, J=8.6 Hz, Ar--H), 7.60 (1H, d, J=2.1 Hz, Ar--H), 8.54 (2H, s, Ar--H).

Provenance & Evidence