Ammonium formate → 1-Azetidin-3-ylmethyl-6-fluoro-1H-indole

HRID 2056380ノート

反応式

HRID 2056380 の反応式
C([N:14]1[CH2:17][CH:16]([CH2:18][N:19]2[C:27]3[C:22](=[CH:23][CH:24]=[C:25]([F:28])[CH:26]=3)[CH:21]=[CH:20]2)[CH2:15]1)(C1C=CC=CC=1)C1C=CC=CC=1.C([O-])=O.[NH4+]>[Pd].C(O)C>[NH:14]1[CH2:17][CH:16]([CH2:18][N:19]2[C:27]3[C:22](=[CH:23][CH:24]=[C:25]([F:28])[CH:26]=3)[CH:21]=[CH:20]2)[CH2:15]1

参加物

5

反応物 2

HCID 2723923Ammonium formateHCID 692042621-(1-benzhydryl-azetidin-3-ylmethyl)-6-fluoro-1H-indole

生成物 1

HCID 218920951-Azetidin-3-ylmethyl-6-fluoro-1H-indole

試薬・触媒・溶媒 2

HCID 23938Palladium触媒HCID 702Ethanol溶媒

実験手順

A mixture of 1-(1-benzhydryl-azetidin-3-ylmethyl)-6-fluoro-1H-indole (0.6 g, 1.6 mmol), palladium on carbon (10%, cat.amount) and ammonium formate (0.2 g, 3.2 mmol) in ethanol (20 mL) was refluxed for 30 min. The mixture was filtered through celite and the solvent removed under vacuum. Diphenylmethane was removed by triturating the residue with ether, methylene chloride and decanting. The remaining product was dried under vacuum. The crude material was directly used in next step without further purification.

後処理

  1. temperaturewas refluxed for 30 min
  2. filtrationThe mixture was filtered through celite
  3. customthe solvent removed under vacuum
  4. customDiphenylmethane was removed
  5. customby triturating the residue with ether, methylene chloride
  6. customdecanting
  7. customThe remaining product was dried under vacuum
  8. customThe crude material was directly used in next step without further purification

出典と根拠

ORDレコード
ord-272f6ed19ac9477c98f984bf8ecfd669
出典データセット
uspto-grants-2008_02
特許番号
US07335666B2

反応ノート

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