Hydrochloric Acid → Methyl 2-(3-fluoro-4-(trifluoromethyl)phenyl)-piperidine-4-carboxylate hydrochloride

HRID 1963224ノート

反応式

HRID 1963224 の反応式
[F:1][C:2]1[CH:3]=[C:4]([C:12]2[CH:13]=[C:14]([CH:19]=[CH:20][N:21]=2)[C:15]([O:17][CH3:18])=[O:16])[CH:5]=[CH:6][C:7]=1[C:8]([F:11])([F:10])[F:9].[ClH:22]>CO.[Pt](=O)=O>[ClH:22].[F:1][C:2]1[CH:3]=[C:4]([CH:12]2[CH2:13][CH:14]([C:15]([O:17][CH3:18])=[O:16])[CH2:19][CH2:20][NH:21]2)[CH:5]=[CH:6][C:7]=1[C:8]([F:11])([F:9])[F:10]

参加物

5

反応物 2

HCID 313Hydrochloric AcidHCID 66732503Methyl 2-(3-fluoro-4-(trifluoromethyl)phenyl)isonicotinate

生成物 1

HCID 66731714Methyl 2-(3-fluoro-4-(trifluoromethyl)phenyl)-piperidine-4-carboxylate hydrochloride収率 94.2%

試薬・触媒・溶媒 2

HCID 345198Adams' catalyst触媒HCID 887Methanol溶媒

実験手順

Methyl 2-(3-fluoro-4-(trifluoromethyl)phenyl)isonicotinate (2.9 g, 9.69 mmol) was dissolved in methanol and hydrogen chloride (1.25 M in methanol, 11.63 mL, 14.54 mmol) was added. The solvent was evaporated and the residue redissolved in methanol (50 mL), platinum(IV) oxide (0.220 g, 0.97 mmol) was added and the reaction mixture was hydrogenated at 5 bar and room temperature in a Büchi hydrogenator for 2 h. The catalyst was removed by filtration and the solvent was evaporated to yield methyl 2-(3-fluoro-4-(trifluoromethyl)phenyl)-piperidine-4-carboxylate hydrochloride (3.12 g, 94%). MS m/z 306 (M+H)+

後処理

  1. customThe solvent was evaporated
  2. dissolutionthe residue redissolved in methanol (50 mL)
  3. customThe catalyst was removed by filtration
  4. customthe solvent was evaporated

出典と根拠

ORDレコード
ord-2e45d39a148d4ddeacffba172e687c9a
出典データセット
uspto-grants-2013_04
特許番号
US08415378B2

反応ノート

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