Trifluoroacetic acid → 3-Phenylazetidin-3-ol; trifluoroacetic acid

HRID 540389ノート

反応式

HRID 540389 の反応式
[F:1][C:2]([F:7])([F:6])[C:3]([OH:5])=[O:4].[OH:8][C:9]1([C:20]2[CH:25]=[CH:24][CH:23]=[CH:22][CH:21]=2)[CH2:12][N:11](C(OC(C)(C)C)=O)[CH2:10]1>ClCCl>[F:1][C:2]([F:7])([F:6])[C:3]([OH:5])=[O:4].[OH:8][C:9]1([C:20]2[CH:25]=[CH:24][CH:23]=[CH:22][CH:21]=2)[CH2:12][NH:11][CH2:10]1

参加物

4

反応物 2

HCID 6422Trifluoroacetic acidHCID 65810524Tert-butyl 3-hydroxy-3-phenylazetidine-1-carboxylate

生成物 1

HCID 669881473-Phenylazetidin-3-ol; trifluoroacetic acid収率 68%

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

1 ml of trifluoroacetic acid is added to a solution containing 50 mg (0.19 mmol) of tert-butyl 3-hydroxy-3-phenylazetidine-1-carboxylate dissolved in 4 ml of dichloromethane. The reaction medium is stirred at ambient temperature for 3 hours and then concentrated. The crude product obtained is purified by silica gel chromatography (eluent 90/10 dichloromethane/methanol). 36 mg in the form of a white powder are obtained with a yield of 68%.

後処理

  1. concentrationconcentrated

出典と根拠

ORDレコード
ord-b86cd5134ced443eaf9959beb2875b9e
出典データセット
uspto-grants-2014_10
特許番号
US08871187B2

反応ノート

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