Hydrazine hydrate (1:1) → Ethyl 4-(aminomethyl)-2-(4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}piperidin-1-yl)-1,3-thiazole-5-carboxylate

Participants

Reaction Steps

Ethyl 2-(4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}piperidin-1-yl)-4-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-1,3-thiazole-5-carboxylate (Example 277; 1.43 g, 2.42 mmol) in EtOH (10 ml) was added hydrazine hydrate (0.174 ml; 3.63 mmol) and refluxed for 14 h. The reaction mixture cooled to room temperature and concentrated in vacuo, diluted with DCM and acidified with 10% HCl, washed with H2O. The precipitate was filtered and dried in vacuo to give the title compound (600 mg).

Provenance & Evidence