Morpholine → HCID 11993495, compound

Participants

Reaction Steps

5-[2-(acetylamino)-4-methyl-1,3-thiazol-5-yl]thiophene-2-sulfonyl chloride, prepared as in Step 1 of example 9 (110 mg; 0.33 mmol; 1 eq.), is dissolved in DCM (10 ml). Morpholine (0.04 ml; 0.46 mmol; 1.40 eq.) and DIEA (0.17 ml; 0.98 mmol; 3 eq.) are added. After one hour, the solvents are evaporated. The crude product is purified by preparative HPLC, affording Compound (13) is obtained as white-off solid (15 mg; 19%). 1H NMR (DMSO-d6) δ 2.15 (s, 3H), 2.46 (s, 3H), 2.96 (m, 4H), 3.67 (m, 4H), 7.33 (d, J=3.8 Hz, 1H), 7.61 (d, J=3.8 Hz, 1H), 12.35 (s, 1H). M−(ESI): 386.17; M+(ESI): 388.46. HPLC, Rt: 3.21 min (purity: 99.7%).

Provenance & Evidence