Lithium Hydroxide → N-(5-(3-(1-(3-fluorobenzyl)-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridin-5-yl)-2-morpholinophenyl)methanesulfonamide

Participants

Reaction Steps

Using similar reaction conditions as described in step-iii of example-1, N-(5-(3-(1-(3-fluorobenzyl)-1H-pyrazol-4-yl)-1-tosyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-2-morpholinophenyl) methanesulfonamide (240 mg, 0.342 mmol) was hydrolyzed by lithium hydroxide (143 mg, 3.42 mmol), THF/Methanol/water (20/8/8 mL) to yield 34 mg (18%) of the titled compound. 1H NMR (DMSO-D6, 400 MHz): δ 11.8 (s, 1H), 8.618 (s, 1H), 8.469-8.464 (m, 1H), 8.421 (s, 1H), 8.317-8.313 (d, 1H), 7.963 (s, 1H), 7.782-7.777 (d, 1H), 7.649-7.645 (d, 1H), 7.58-7.52 (m, 1H), 7.44-7.366 (m, 2H), 7.16-7.08 (m, 3H), 5.402 (s, 2H), 3.80.3-3.791 (m, 4H), 3.197 (s, 3H), 2.898-2.887 (m, 4H). MS: m/z=546.8 (M+1); HPLC: 96.04% in method B.

Provenance & Evidence