Hydrochloric Acid → 4-((2,2,2-Trifluoroethoxy)methyl)piperidine hydrochloride

反応式

[ClH:1].O1CCOCC1.[F:8][C:9]([F:27])([F:26])[CH2:10][O:11][CH2:12][CH:13]1[CH2:18][CH2:17][N:16](C(OC(C)(C)C)=O)[CH2:15][CH2:14]1>>[ClH:1].[F:27][C:9]([F:8])([F:26])[CH2:10][O:11][CH2:12][CH:13]1[CH2:18][CH2:17][NH:16][CH2:15][CH2:14]1

参加物

反応物 3

HCID 313Hydrochloric Acid

HCID 312751,4-Dioxane

HCID 66802837Tert-butyl 4-[(2,2,2-trifluoroethoxy)methyl]piperidine-1-carboxylate2 回

生成物 1

HCID 457917814-((2,2,2-Trifluoroethoxy)methyl)piperidine hydrochloride収率 59%

実験手順

A solution of 4M hydrogen chloride in 1,4-dioxane (2.48 mL, 9.93 mmol) was added to tert-butyl 4-[(2,2,2-trifluoroethoxy)methyl]piperidine-1-carboxylate (Intermediate 180, 0.289 g, 0.993 mmol) and the mixture was stirred at room temperature for 18 h before being evaporated to dryness to provide the title compound (0.136 g, 59%). Method B HPLC-MS: MH+ (HCl salt) requires m/z=198 Found: m/z=198, Rt=0.72 min.