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HRID 389571作成日:2026年10月26日

2-Methylpropyl isocyanate → 4-[4-(7-Amino-2-benzo[d]isothiazol-7-yl-furo[2,3-c]pyridin-4-yl)-pyrazol-1-yl]-piperidine-1-carboxylic acid isobutyl-amide

https://huagongshe.com/reaction/389571

反応式

関与物質

役割名称HCID仕込み量
反応物2-Methylpropyl isocyanateHCID 61281—
反応物DiisopropylethylamineHCID 81531—
反応物2-benzo[d]isothiazol-7-yl-4-(1-piperidin-4-yl-1H-pyrazol-4-yl)-furo[2,3-c]pyridin-7-ylamineHCID 66759914—
溶媒DimethylformamideHCID 6228—
生成物4-[4-(7-Amino-2-benzo[d]isothiazol-7-yl-furo[2,3-c]pyridin-4-yl)-pyrazol-1-yl]-piperidine-1-carboxylic acid isobutyl-amideHCID 66759617—

反応手順

To a solution of 2-benzo[d]isothiazol-7-yl-4-(1-piperidin-4-yl-1H-pyrazol-4-yl)-furo[2,3-c]pyridin-7-ylamine (20.8 mg, 0.05 mmol) in DMF (0.5 mL) was added diisopropylethylamine (0.05 mL, 6.5 mmol) and isobutyl isocyanate (0.06 mmol). The resulting solution stirred at room temperature overnight. The mixture was concentrated and then purified by MDP to afford the title compound as an off-white solid. 1H NMR (400 MHz, CD3OD): δ 9.51 (s, 1H), 9.12 (d, J=1.5 Hz, 1H), 8.84 (d, J=7.3 Hz, 1H), 8.72 (d, J=7.3 Hz, 1H), 8.35 (s, 1H), 8.07 (s, 1H), 7.92 (s, 1H), 7.88 (s, 1H), 4.53 (m, 1H), 3.03 (m, 4H), 2.18 (m, 2H), 2.06 (m, 4H), 1.83 (m, 1H), 1.76 (d, J=5.8 Hz, 6H); MS (ESI): MS (ESI): 516.64 [M+H]+; HPLC tR=0.86 min (HPLC: Analytical—2 min).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08378104B2
出典データセットuspto-grants-2013_02
ORD IDord-6c1130ec905043dd9500c966d7d8dade
出典メモuspto-grants-2013_02