Trifluoroacetic acid → (1R,5R)-7-Fluoro-4-oxo-3-[(1R)-1-phenylethyl]-3-azabicyclo[3.3.0]octan-1-ylcarboxylic acid

HRID 1917345ノート

反応式

HRID 1917345 の反応式
C([O:5][C:6]([C@:8]12[CH2:15][CH:14]([F:16])[CH2:13][C@H:12]1[C:11](=[O:17])[N:10]([C@@H:18]([C:20]1[CH:25]=[CH:24][CH:23]=[CH:22][CH:21]=1)[CH3:19])[CH2:9]2)=[O:7])(C)(C)C.FC(F)(F)C(O)=O>C(Cl)Cl>[F:16][CH:14]1[CH2:15][C@@:8]2([C:6]([OH:7])=[O:5])[C@H:12]([C:11](=[O:17])[N:10]([C@@H:18]([C:20]3[CH:25]=[CH:24][CH:23]=[CH:22][CH:21]=3)[CH3:19])[CH2:9]2)[CH2:13]1

参加物

4

反応物 2

HCID 6422Trifluoroacetic acidHCID 67491056(1R,5R)-7-Fluoro-4-oxo-3-[(1R)-1-phenylethyl]-3-azabicyclo[3.3.0]octan-1-ylcarboxylic acid tert-butyl ester

生成物 1

HCID 67490956(1R,5R)-7-Fluoro-4-oxo-3-[(1R)-1-phenylethyl]-3-azabicyclo[3.3.0]octan-1-ylcarboxylic acid

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

(1R,5R)-7-Fluoro-4-oxo-3-[(1R)-1-phenylethyl]-3-azabicyclo[3.3.0]octan-1-ylcarboxylic acid tert-butyl ester (705 mg, 2.03 mmol) was dissolved in methylene chloride (4 mL). Trifluoroacetic acid (4 mL) was added under ice-cooling, and then the mixture was stirred at room temperature for one hour. The reaction solution was concentrated under reduced pressure. Toluene was added to the residue, and the mixture was concentrated under reduced pressure again to give 595 mg (quantitative) of the title compound as a white solid.

後処理

  1. temperaturecooling
  2. concentrationThe reaction solution was concentrated under reduced pressure
  3. additionToluene was added to the residue
  4. concentrationthe mixture was concentrated under reduced pressure again

出典と根拠

ORDレコード
ord-68e2c99235874cdaa4ec28511b326420
出典データセット
uspto-grants-2013_12
特許番号
US08618094B2

反応ノート

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