Lithium hydroxide, monohydrate → N-(3-{3-[2-(1,2,3,4-tetrahydro-7-isoquinolinylamino)-4-pyrimidinyl]-pyrazolo[1,5-a]pyridin-2-yl}phenyl)benzamide

関与物質

反応手順

To a solution of N-{3-[3-(2-{[2-(2,2,2-Trifluoroacetyl)-1,2,3,4-tetrahydro-7-isoquinolinyl]amino}-4-pyrimidinyl)pyrazolo[1,5-a]pyridin-2-yl]phenyl}benzamide (191 mg, 0.30 mmol) in THF (4.0 mL) was added a solution of LiOH.H2O (19.8 mg, 0.47 mmol) in H2O (1.5 mL). The mixture was stirred at rt for 30 min. The mixture was partitioned between saturated aq. NaHCO3 and 5:1 CHCl3/isopropanol. The organic layer was separated, dried over Na2SO4, filtered and concentrated to give 191 mg of crude product. Purification by silica gel chromatography (0 to 40% sat. ammonia/MeOH in EtOAc) afforded 163.2 mg of the title compound as a white powder. LCMS ((ES)+ 538.3. 1H NMR (400, DMSO-d6) δ 2.63 (t, 2H, J=5.6), 2.96 (t, 2H, J=5.6), 3.80 (s, 2H), 6.46 (d, 1H, J=5.2), 6.95 (d, 1H, J-=8.4), 7.11 (t, 1H, J=6.4), 7.29 (d, 1H, J=8.0), 7.36 (d, 1H, J=9.2), 7.43-7.57 (m, 5H), 7.93 (d, 2H, J=7.2), 8.09 (s, 1H), 8.21 (d, 1H, J=5.6), 8.49 (d, 1H, J=8.8), 8.82 (d, 1H, J=6.8), 9.41 (s, 1H), 10.37 (s, 1H).

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