Methanol → HCID 89649130、化合物

反応式

[CH2:1]([O:3][C:4]1[CH:5]=[CH:6][C:7]([F:21])=[C:8]([C:10]2[CH:15]=[C:14]([CH:16]([CH3:18])[CH3:17])[N:13]=[C:12]([C:19]#N)[CH:11]=2)[CH:9]=1)[CH3:2].[O:22]1CCOC[CH2:23]1.C[OH:29]>Cl>[CH2:1]([O:3][C:4]1[CH:5]=[CH:6][C:7]([F:21])=[C:8]([C:10]2[CH:15]=[C:14]([CH:16]([CH3:18])[CH3:17])[N:13]=[C:12]([C:19]([O:22][CH3:23])=[O:29])[CH:11]=2)[CH:9]=1)[CH3:2]

参加物

実験手順

A mixture of 4-(5-ethoxy-2-fluoro-phenyl)-6-isopropyl-pyridine-2-carbonitrile (which may be prepared as described in Description 114) (1.09 g, 3.8 mmol) in 4M HCl in dioxan (12 mL, 48 mmol) and methanol (12 mL) was heated to reflux under nitrogen overnight. The solvents were evaporated and ethyl acetate (150 ml) and NaHCO3 solution (150 ml) were added. The product was extracted into ethyl acetate (3 x) and the extracts were dried (Na2SO4) and concentrated. Chromatography (0-10% diethyl ether in DCM) gave methyl 4-(5-ethoxy-2-fluoro-phenyl)-6-isopropyl-pyridine-2-carboxylate (D115) (730.8 mg);