Trifluoroacetic acid → N-[(1S,2S,5R)-7-methyl-3-aza-bicyclo[3.3.0]oct-2-ylmethyl]-2,2,2-trifluoro-acetamide

HRID 425800ノート

反応式

HRID 425800 の反応式
C(OC([N:8]1[CH2:15][C@H:14]2[C@H:10]([CH2:11][CH:12]([CH3:16])[CH2:13]2)[C@H:9]1[CH2:17][NH:18][C:19](=[O:24])[C:20]([F:23])([F:22])[F:21])=O)(C)(C)C.C(O)(C(F)(F)F)=O>C(Cl)Cl>[CH3:16][CH:12]1[CH2:11][C@H:10]2[C@H:14]([CH2:15][NH:8][C@@H:9]2[CH2:17][NH:18][C:19](=[O:24])[C:20]([F:23])([F:21])[F:22])[CH2:13]1

参加物

4

反応物 2

HCID 6422Trifluoroacetic acidHCID 86643543(1S,2S,5R)-2-[(2,2,2-trifluoro-acetylamino)-methyl]-7-methyl-3-aza-bicyclo[3.3.0]-octane-3-carboxylic acid tert.-butyl ester

生成物 1

HCID 86643544N-[(1S,2S,5R)-7-methyl-3-aza-bicyclo[3.3.0]oct-2-ylmethyl]-2,2,2-trifluoro-acetamide

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

To a cold (0° C.) solution of (1S,2S,5R)-2-[(2,2,2-trifluoro-acetylamino)-methyl]-7-methyl-3-aza-bicyclo[3.3.0]-octane-3-carboxylic acid tert.-butyl ester (1.51 g) in DCM (13 mL) was slowly added TFA (3.31 mL, 10 eq). The reaction mixture was allowed to warm at RT and stirred overnight. Solvent and excess of TFA were removed in vacuo and the product was used for the next step without further purification.

後処理

  1. customSolvent and excess of TFA were removed in vacuo
  2. customthe product was used for the next step without further purification

出典と根拠

ORDレコード
ord-09f31d8d967e47e9a5c4fb78cc1b43ed
出典データセット
uspto-grants-2012_01
特許番号
US08106215B2

反応ノート

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