TBAF tetrahydrofuran → HCID 178480848, compound

Participants

Reaction Steps

To 80 mL of THF, 5-[5-(4-methylpiperazinyl)methyl[1,3,4]oxadiazol-2-yl]-2-[2-(4-pyridyl)ethylamino]-4-(2-trimethylsilylethoxy)pyrimidine (3.83 g, 7.71 mmol) obtained in Step 3 was dissolved, then TBAF-THF solution (1.0 mol/L, 15.8 mL, 15.8 mmol) was added thereto, followed by stirring at a temperature between room temperature and 50° C. in total of 5 hours. After completion of the reaction was confirmed by thin-layer chromatography, the reaction mixture was concentrated under reduced pressure and the residue was purified by silica gel column chromatography (chloroform/methanol). Then, the residue was crystallized from hexane/ethyl acetate to give 4-hydroxy-5-[5-(4-methylpiperazinyl)methyl[1,3,4]oxadiazol-2-yl]-2-[2-(4-pyridyl)ethylamino]pyrimidine [Compound (AB) in which R2B is [2-(4-pyridyl)ethylamino] and —X—Y—Z— is

Provenance & Evidence