反应详情

A solution of (E)-3-(4-acetyl-2,3,4,5-tetrahydro-1H-pyrido[2,3-e][1,4]diazepin-7-yl)-N-methyl-N-(3-methylbenzofuran-2-ylmethyl)acrylamide (89 mg, 0.21 mmol) in CH2Cl2 (4 mL) was treated with anhydrous HCl (0.21 mL of a 1.0 M solution in Et2O, 0.21 mmol). After stirring for 15 min, the mixture was diluted with Et2O (25 mL) and allowed to stir for 2 h. The solid was isolated by filtration, washed with Et2O, and dried under vacuum at 50° C. for 3 days to give the title compound (83 mg, 88%) as a white powder and as a mixture of amide rotamers: 1H NMR (300 MHz, DMSO-d6) δ 8.46-8.23 (m, 3H), 7.58-7.22 (m, 6H), 5.02-4.80 (m, 4H), 3.87-3.74 (m, 4H), 3.19-2.90 (m, 3H), 2.26 (s, 3H), 2.03-1.99 (m, 3H); MS (ESI) m/e 419 (M+H)+.

1. stirringto stir for 2 h
2. customThe solid was isolated by filtration
3. washwashed with Et2O
4. customdried under vacuum at 50° C. for 3 days