Hydrochloric Acid → (4-Iodo-phenyl)-[4-((R)-1-pyrrolidin-2-ylmethoxy)-phenyl]-methanone

Participants

Reaction Steps

To a 20 mL vial which contained a solution of the product from step 2 (25 mg, 0.05 mmol) in dioxane (1 mL) was added HCl (4 N in dioxane, 2 mL) at 0° C. The mixture was allowed to warm to rt and stir at rt for 16 h. The solvent was reduced to 1 mL and ether (15 mL) was added to this vial. The resulting solid was filtered out and dried under vacuo to yield the title product (16 mg, 80%); LCMS; 100% ESI+ Calcd: 407.3, found m/z: 408.5 (M+1); 1H NMR (500 MHz, DMSO-d6); δ 1.71-1.80 (m, 1H), 1.82-2.06 (m, 2H), 2.10-2.20 (m, 1H), 3.16-3.30 (m, 2H), 3.90-4.00 (m, 1H), 4.23-4.27 (m, 1H), 4.38 (dd, J1=10.0 Hz, J2=2.5 Hz, 1H), 7.14 (d, J=8.5 Hz, 2H), 7.46 (d, J=7.5 Hz, 2H), 7.78 (d, J=9.0 Hz, 2H), 7.95 (d, J=8.0 Hz, 2H):

Provenance & Evidence