Hydrochloric Acid → HCID 131734229, compound

Participants

Reaction Conditions

Reaction Steps

Chiral-tert-butyl 5′-(5-(3,5-dichloro-4-fluorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)-3′H-spiro[azetidine-3,1′-isobenzofuran]-1-carboxylate (Preparation 5, 1.1 g, 2.0 mmol) was dissolved in methanol (50 mL). A methanolic solution of HCl (5 mL of a 1.25M solution) was added and the reaction was heated to 65° C. for 18 hours. The reaction was cooled and concentrated under vacuum to afford the intermediate (980 mg, 100%) a solid. 1H NMR, 300 MHz (d6-DMSO) δ ppm: 9.86 (1H), 9.45 (1H), 8.14 (1H), 7.82 (3H), 7.70 (1H), 5.15 (2H), 4.41-4.30 (6H); m/z (CI) 461 [M+H] (free amine). The asterisk (*) depicts a chiral center.

Provenance & Evidence