反应详情

Palladium hydroxide (0.092 mmol, 12.96 mg) was wetted with a small volume of water before addition of (S)-ethyl 1-((2-(benzyloxycarbonylamino)-2,3-dihydro-1H-inden-5-yl)methyl)-5-(trifluoromethyl)-1H-pyrazole-4-carboxylate (0.092 mmol, 45 mg) in Ethanol (5 mL). A small volume DCM was added to aid solubility. Aq. HCl 5N (0.500 ml) was added before the mixture was left to stand at room temp for around 1.5 h before hydrogenating at 2 bar for 45 min. After this time, the mixture was filtered through a filter tip and concentrated to give the desired product as a colourless oil (36 mg, 0.092 mmol, 100%). 1H NMR (400 MHz, CD3OD) δ 1.33 (t, 3H) 2.98 (m, 2H) 3.40 (m, 2H) 4.10 (m, 1H) 4.31 (q, 2H) 5.50 (s, 2H) 7.05 (d, 1H), 7.10 (s, 1H), 7.27 (d, 1H) 8.04 (s, 1H).

1. waitwas left
2. filtrationAfter this time, the mixture was filtered through a filter tip
3. concentrationconcentrated