Hydrochloric Acid → 2-(3,5-dichlorophenylamino)-1-((S)-3-aminopiperidin-1-yl)ethanone
反応式
[Cl:1][C:2]1[CH:3]=[C:4]([NH:9][CH2:10][C:11]([N:13]2[CH2:18][CH2:17][CH2:16][C@H:15]([NH:19]C(=O)OC(C)(C)C)[CH2:14]2)=[O:12])[CH:5]=[C:6]([Cl:8])[CH:7]=1.Cl>O1CCOCC1>[Cl:1][C:2]1[CH:3]=[C:4]([NH:9][CH2:10][C:11]([N:13]2[CH2:18][CH2:17][CH2:16][C@H:15]([NH2:19])[CH2:14]2)=[O:12])[CH:5]=[C:6]([Cl:8])[CH:7]=1参加物
4
実験手順
To a solution of tert-butyl(S)-1-(2-(3,5-dichlorophenylamino)acetyl)piperidin-3-ylcarbamate (0.9 mg, 2.2 mmol) in 1,4-dioxane (5 mL) was added 4 N HCl in dioxane (10 mL) and the reaction mixture was stirred for 1 h. The reaction mixture was concentrated in vacuo and the resultant residue was dissolved in water and aqueous phase was adjusted to a pH 9 with sat. NaHCO3 and extracted with EtOAc (3×50 mL). The combined organic layer was dried over Na2SO4 and evaporated in vacuo to afford the titled intermediate (540 mg, 79%), which was used in the next step without purification. LCMS: m/z: [M+1]=302.