反应详情

A solution of N-(3-(1-(2-hydroxyethyl)-1,2,3,6-tetrahydropyridin-4-yl)-1H-indol-5-yl)thiophene-2-carboximidamide (0.125 g, 0.341 mmol) in dry methanol (3 mL) was treated with hydrogen chloride (1M in diethyl ether) (1.023 mL, 1.023 mmol) at room temperature. Solvent was evaporated under reduced pressure after stirring for 15 minutes and the crude material was dried to obtain N-(3-(1-(2-hydroxyethyl)-1,2,3,6-tetrahydropyridin-4-yl)-1H-indol-5-yl)thiophene-2-carboximidamide dihydrochloride (0.14 g, 93%) as a solid. 1H NMR (DMSO-d6) δ 11.70 (s, 1H), 11.47 (s, 1H), 10.57 (brs, 1H), 9.66 (s, 1H), 8.61 (s, 1H), 8.19-8.16 (m, 2H), 7.94 (s, 1H), 7.68 (d, 1H, J=2.1 Hz), 7.59 (d, 1H, J=8.4 Hz), 7.39 (t, 1H, J=4.5 Hz), 7.18 (d, 1H, J=9.3 Hz), 6.16 (s, 1H), 5.36 (s, 1H), 4.06-3.96 (m, 1H), 3.90-3.80 (m, 3H), 3.71-3.67 (m, 1H), 3.28-3.0 (m, 2H), 2.98-2.91 (m, 1H), 2.81-2.72 (m, 1H), 2.50-2.40 (m, 2H, merged with DMSO peak); ESI-MS (m/z, %): 367 (MH+, 39), 294 (100); ESI-HRMS calculated for C20H23N4OS (MH+, free base), calculated: 367.1587; observed: 367.1605.

1. customSolvent was evaporated under reduced pressure
2. dry with materialthe crude material was dried