1-Butanol → 1-(4-((4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrimidin-2-ylamino)methyl)-1H-indol-3-yl)-2,2,2-trifluoroethanone

関与物質

反応条件

反応手順

A vial was charged with 53 (300 mg, 1.27 mmol), (1H-indol-4-yl)methanamine (279 mg, 1.903.20 mmol, CASRN 3468-18-6), DIPEA (0.67 mL) and n-BuOH (3 mL), sealed and heated at 140 C for 72 h. The reaction mixture was concentrated in vacuo, and the residue was partitioned between EtOAc and H2O. The aqueous layer was extracted once with EtOAc. The combined organic extracts were dried (Na2SO4), filtered and concentrated in vacuo. The crude produce was directly dissolved in TFA (3 mL), and the mixture was heated at 70° C. for 2 h. The reaction mixture was concentrated under reduced pressure and the residue purified by preparative HPLC to afford 38.3 mg (7%) of I-37.

情報源と証拠