Dichloromethane → HCID 66893894, compound

Participants

Reaction Steps

tert-Butyl methyl[3-(methyl{5-[(phenylsulfonyl)amino]-1-benzofuran-7-yl}amino)propyl]carbamate (Intermediate 3; 202 mg, 0.43 mmol) in DCM (2 mL) was treated with TFA (2 mL) at 0° C. for 10 min and was stirred for an additional 30 min at room temperature. After concentration in vacuo, the residue was re-dissolved in MeOH and treated with an excess of 1M HCl in diethyl ether. Removal of the solvents gave the title compound (173 mg, 98%) as a white solid; HPLC 100%, RT: 1.65 min (System A); 100%, RT: 0.630 min (System B); 1H NMR (methanol-d4) δ ppm 1.85-2.00 (m, 2H), 2.67 (s, 3H), 3.04-3.17 (m, 5H), 3.64-3.73 (m, 2H), 6.81-6.84 (m, 1H), 6.95-6.98 (m, 1H), 7.06-7.09 (m, 1H), 7.43-7.60 (m, 3H), 7.72-7.78 (m, 2H), 7.81-7.85 (m, 1H); MS m/z 374 (M+H)+.

Provenance & Evidence