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HRID 1159884作成日:2026年10月25日

Lithium Hydroxide → 4-[2-(3-aminophenyl)pyrazolo[1,5-a]pyridin-3-yl]-N-(3-fluorophenyl)-2-pyrimidinamine

https://huagongshe.com/reaction/1159884

反応式

関与物質

役割名称HCID仕込み量
反応物Lithium HydroxideHCID 3939—
反応物2,2,2-Trifluoro-N-[3-(3-{2-[(3-fluorophenyl)amino]-4-pyrimidinyl}pyrazolo-[1,5-a]pyridin-2-yl)phenyl]acetamideHCID 59513829—
溶媒WaterHCID 962—
溶媒TetrahydrofuranHCID 8028—
生成物4-[2-(3-aminophenyl)pyrazolo[1,5-a]pyridin-3-yl]-N-(3-fluorophenyl)-2-pyrimidinamineHCID 59511403—

反応手順

A solution of 2,2,2-trifluoro-N-(3-{3-[2-(3-fluoro-phenylamino)-pyrimidin-4-yl]-pyrazolo[1,5-a]pyridin-2-yl}-phenyl)-acetamide (2.15 g, 4.4 mmol) and lithium hydroxide (277 mg, 6.6 mmol) in THF (44 mL) and water (10 mL) was stirred for 16 h. The reaction was extracted with DCM. The combined organic phases were dried over MgSO4 and purified through silica gel to give the title compound as a white solid. 1H NMR (400 MHz, d6-DMSO): δ 9.75 (s, 1H), 8.78 (d, J=6.8 Hz, 1H), 8.52 (d, J=9.2 Hz, 1H), 8.25 (d, J=5.6 Hz, 1H), 7.80 (d, J=12.4 Hz, 1H), 7.47-7.43 (m, 2H), 7.29-7.23 (m, 1H), 7.12-7.06 (m, 2H), 6.77 (s, 1H), 6.71 (dt, J=8.4 and 2.4 Hz, 1H), 6.66-6.62 (m, 2H), 6.54 (d, J=5.6 Hz, 1H), 5.21 (s, 2H) ppm. HRMS calculated C23H17FN6 [M+H]+ 397.1577 found 397.1558.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07812022B2
出典データセットuspto-grants-2010_10
ORD IDord-a8fd79a0571f4466bbfa8da77732e6d9
出典メモuspto-grants-2010_10