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HRID 19516作成日:2026年10月26日

Picolinic acid → 4-Amino-2-methyl-N-(4-{[(2-pyridinylcarbonyl)amino]methyl}phenyl)-6-quinolinecarboxamide

https://huagongshe.com/reaction/19516

反応式

関与物質

役割名称HCID仕込み量
反応物Picolinic acidHCID 1018—
反応物TriethylamineHCID 8471—
反応物PyBroPHCID 2733179—
反応物4-{[(4-Amino-2-methyl-6-quinolinyl)carbonyl]amino}benzylamineHCID 17864630—
溶媒DimethylformamideHCID 6228—
生成物4-Amino-2-methyl-N-(4-{[(2-pyridinylcarbonyl)amino]methyl}phenyl)-6-quinolinecarboxamideHCID 997898636%

反応手順

To a solution of 27 mg (0.05 mmol) 4-amino-N-[4-(aminomethyl)phenyl]-2-methyl-6-quinolinecarboxamide, 7 mg (0.1 mmol) 2-pyridinecarboxylic acid, and 0.028 ml (0.2 mmol) triethylamine in 2 ml DMF was added 36 mg (0.75 mmol) PyBrop and stirred at room temperature for 1 d. After evaporation of the solvent the residue was purified by HPLC and lyophilized to yield 7.4 mg (23%) of the title compound. MS 412.3 (M+1)+, 1H-NMR (DMSO-d6) δ 2.60 (s, 3H), 4.47 (d, 2H), 6.64 (s, 1H), 7.33 (d, 2H), 7.60 (m, 1H), 7.70 (d, 2H), 7.86 (d, 1H), 8.00 (t, 1H), 8.04 (t, 1H), 8.35 (d, 1H), 8.65 (m, 1H), 8.94 (s, 1H), 8.98 (br. 2H), 9.32 (t, 1H).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07745443B2
出典データセットuspto-grants-2010_06
ORD IDord-11e0391bf0084825be840fd184bdb1a1
出典メモuspto-grants-2010_06