反应详情

To a stirred solution of N-(8-fluoro-1-(2-(methylamino)ethyl)-1,2,3,4-tetrahydroquinolin-6-yl)thiophene-2-carboximidamide (57 mg, 0.171 mmol) in Methanol (3 ml) was added hydrogen chloride, 1M in diethyl ether (0.514 ml, 0.514 mmol). The resulting solution was then concentrated to give the desired N-(8-fluoro-1-(2-(methylamino)ethyl)-1,2,3,4-tetrahydroquinolin-6-yl)thiophene-2-carboximidamide dihydrochloride (69 mg, 0.170 mmol, 99% yield). 1H NMR (DMSO-d6) δ 9.79 (s, 1H); 9.13 (brs, 2H); 8.84 (s, 1H); 8.16 (d, J=4.8 Hz); 7.37 (t, J=4.3 Hz, 1H); 7.14 (d, J=14 Hz, 1H); 6.94 (s, 1H); 3.47-3.40 (m, 2H); 3.24-3.18 (m, 2H); 3.18-3.10 (m, 2H); 2.76 (t, J=6 Hz, 2H); 2.58 (t, J=5.1 Hz, 3H); 1.85-1.78 (m, 2H). EI-MS (m/z, %): 332 (M+, 9); 288 (100). HRMS calculated for C17H21FN4S (M+), calculated: 332.1477, observed: 332.1471. HPLC purity: 95%.

1. concentrationThe resulting solution was then concentrated