Ethyl trifluoroacetate → (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

HRID 425799ノート

反応式

HRID 425799 の反応式
[F:1][C:2]([F:9])([F:8])[C:3]([O:5]CC)=O.[C:10]([O:14][C:15]([N:17]1[CH2:24][C@H:23]2[C@H:19]([CH2:20][CH:21]([CH3:25])[CH2:22]2)[C@H:18]1[CH2:26][NH2:27])=[O:16])([CH3:13])([CH3:12])[CH3:11]>C1COCC1>[C:10]([O:14][C:15]([N:17]1[CH2:24][C@H:23]2[C@H:19]([CH2:20][CH:21]([CH3:25])[CH2:22]2)[C@H:18]1[CH2:26][NH:27][C:3](=[O:5])[C:2]([F:1])([F:8])[F:9])=[O:16])([CH3:12])([CH3:13])[CH3:11]

参加物

4

反応物 2

HCID 9794Ethyl trifluoroacetateHCID 59411604(1S,2S,5R)-2-aminomethyl-7-methyl-3-aza-bicyclo[3.3.0]-octane-3-carboxylic acid tert.-butyl ester

生成物 1

HCID 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

試薬・触媒・溶媒 1

HCID 8028Tetrahydrofuran溶媒

実験手順

Ethyl trifluoroacetate (0.7 mL, 1.4 eq) was added to a solution of (1S,2S,5R)-2-aminomethyl-7-methyl-3-aza-bicyclo[3.3.0]-octane-3-carboxylic acid tert.-butyl ester (1.1 g) in dry THF (14 mL). The reaction mixture was stirred at RT for 1 h. Solvent and excess ethyl trifluoroacetate were evaporated in vacuo. The resulting product was then used for the next step without purification

後処理

  1. customSolvent and excess ethyl trifluoroacetate were evaporated in vacuo
  2. customThe resulting product was then used for the next step without purification

出典と根拠

ORDレコード
ord-8a7c1d34377e492a85e0fbc3ecbd2260
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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