反应详情

(S)-tert-Butyl 2-(4-chlorophenyl)-3-(4-(5-isopropoxy-1H-pyrrolo[2,3-b]pyridin-4-yl)piperazin-1-yl)-3-oxopropyl(isopropyl)carbamate (30 mg, 0.051 mmol) in TFA (3 mL) was stirred for 30 minutes and then concentrated to dryness. The resulting residue was dissolved in minimal DCM (0.2 mL) and added to 2N HCl in ether. The resulting solid was filtered and dried under nitrogen to yield (S)-2-(4-chlorophenyl)-1-(4-(5-isopropoxy-1H-pyrrolo[2,3-b]pyridin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one (15 mg, 60% yield) hydrochloride as a solid. 1H NMR (400 MHz, DMSO-d6) δ 12.30 (s, 1H), 9.23 (s, 1H), 8.56 (s, 1H), 7.99 (s, 1H), 7.51-7.47 (m, 2H), 7.44-7.39 (m, 3H), 6.69 (s, 1H), 4.76 (m, 1H), 4.43 (m, 1H), 3.85-3.50 (m, 7H), 3.47-3.40 (m, 1H), 3.35-3.27 (m, 1H), 3.23-3.15 (m, 1H), 3.05-2.98 (m, 1H), 1.28-1.20 (m, 12H); m/z (ESI pos) 484.4 (100%) [M].

1. concentrationconcentrated to dryness
2. dissolutionThe resulting residue was dissolved in minimal DCM (0.2 mL)
3. additionadded to 2N HCl in ether
4. filtrationThe resulting solid was filtered
5. customdried under nitrogen