Lithium Hydroxide → 5-(3-(1-(3,5-difluorobenzyl)-3,5-dimethyl-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridin-5-yl)-2-methoxy-N-methylbenzenesulfonamide

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Reaction Steps

Using similar reaction conditions as described in step-iii of example 1, 5-(3-(1-(2,5-difluorobenzyl)-3,5-dimethyl-1H-pyrazol-4-yl)-1-tosyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-2-methoxy-N-methylbenzenesulfonamide (180 mg, 0.2604 mmol) was hydrolyzed by lithium hydroxide (109 mg, 2.604 mmol), THF/Methanol/water (24/12/6 ml) to yield 16 mg (11.4% yield) of the titled compound after purification by preparative TLC (SiO2-1000 micron eluted by 3% MeOH in CHCl3). 1H NMR (CD3OD, 300 MHz): δ 8.382 (m, 1H), 7.940-7.935 (d, 1H), 7.816-7.779 (m, 2H), 7.342 (s, 1H), 7.241-7.213 (d, 1H), 6.68-6.64 (m, 1H), 5.275 (s, 2H), 3.914 (s, 3H), 2.441 (s, 3H), 2.128-2.101 (d, 6H). MS: m/z=538.1 (M+1); HPLC: 95.69% in method B.

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