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HRID 887193作成日:2026年10月27日

4-Morpholinobenzylamine → N-5-isoquinolinyl-N'-[4-(4-morpholinyl)benzyl]urea

https://huagongshe.com/reaction/887193

反応式

関与物質

役割名称HCID仕込み量
反応物4-MorpholinobenzylamineHCID 2776458—
反応物5-IsocyanatoisoquinolineHCID 11586357—
溶媒Diethyl EtherHCID 3283—
生成物N-5-isoquinolinyl-N'-[4-(4-morpholinyl)benzyl]ureaHCID 10248092—

反応手順

The product from Example 66B (285 mg, 1.48 mmol) in diethyl ether (10 mL) was treated with the product from Example 61A. The mixture was filtered and the filter cake purified by chromatography (95:5 CH2Cl2-MeOH, eluant) to provide that title compound as a white solid. The corresponding di-hydrochloride salt was prepared using methanolic HCl to afford a yellow solid (505 mg, 78%). 1H NMR (300 MHz, DMSO-d6) δ 9.26 (s, 1H), 8.67 (s, 1H), 8.52-8.55 (m, 1H), 8.32 (dd, J=7.8 Hz, 1.1 Hz, 1H), 7.92 (d, J=6.1 Hz, 1H), 7.73 (d, J=8.2 Hz, 1H), 7.60 (m, 1H), 7.23 (d, J=8.8 Hz, 2H), 6.92-6.96 (m, 3H), 4.26 (d, 5.4 Hz, 2H), 3.72-3.75 (m, 4H), 3.06-3.12 (m, 4H); MS (ESI+) m/z 363 (M+H)+.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08247413B2
出典データセットuspto-grants-2012_08
ORD IDord-84f8566165734de08f4524d93fdbfc88
出典メモuspto-grants-2012_08