4-Methylmorpholine → Pyridine-2-carboxylic acid 4-hydroxymethyl-benzylamide

関与物質

役割	名称	HCID	仕込み量
反応物	4-Methylmorpholine	HCID 7972	—
反応物	1-Hydroxybenzotriazole	HCID 75771	—
反応物	1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride	HCID 2723939	—
反応物	[4-(Aminomethyl)phenyl]methanol	HCID 6496943	—
生成物	Pyridine-2-carboxylic acid 4-hydroxymethyl-benzylamide	HCID 22601292	95%

反応手順

Using General Procedure F: Reaction of (4-aminomethyl-phenyl)-methanol (200 mg, 1.46 mmol, 1-hydroxybenzotriazole (218 mg, 1.61 mmol), 4-methyl morpholine (241 μL, 2.19 mmol), and EDCl (309 mg, 1.61 mmol) for 2 h at room temperature gave the title compound (335 mg, 95%) as a yellow oil. 1H NMR (300 MHz, CDCl3) δ 4.67 (d, 2H, J=6.0 Hz), 4.69 (s, 2H), 7.36 (br s, 4H), 7.43-7.44 (m, 1H), 7.85-7.86 (m, 1H), 8.24 (d, 1H, J=9.0 Hz), 8.52 (br s, 1H), 8.52 (d, 1H, J=3.0 Hz). ES-MS m/z 243 (M+H).

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US06835731B2
出典データセット	uspto-grants-2004_12
ORD ID	ord-5a4585a53312435aa88defc2671842d6
出典メモ	uspto-grants-2004_12