(R)-[4-(3-isopropenyl-5-trifluoromethyl-benzenesulfonylamino)-4,5,6,7-tetrahydro-indazol-1-yl]-acetic acid ethyl ester → (R)-[4-(3-isopropyl-5-trifluoromethyl-benzenesulfonylamino)-4,5,6,7-tetrahydro-indazol-1-yl]-acetic acid ethyl ester

HRID 1645164ノート

反応式

HRID 1645164 の反応式
[CH2:1]([O:3][C:4](=[O:32])[CH2:5][N:6]1[C:14]2[CH2:13][CH2:12][CH2:11][C@@H:10]([NH:15][S:16]([C:19]3[CH:24]=[C:23]([C:25]([F:28])([F:27])[F:26])[CH:22]=[C:21]([C:29]([CH3:31])=[CH2:30])[CH:20]=3)(=[O:18])=[O:17])[C:9]=2[CH:8]=[N:7]1)[CH3:2]>CO.[Pd]>[CH2:1]([O:3][C:4](=[O:32])[CH2:5][N:6]1[C:14]2[CH2:13][CH2:12][CH2:11][C@@H:10]([NH:15][S:16]([C:19]3[CH:24]=[C:23]([C:25]([F:27])([F:28])[F:26])[CH:22]=[C:21]([CH:29]([CH3:31])[CH3:30])[CH:20]=3)(=[O:18])=[O:17])[C:9]=2[CH:8]=[N:7]1)[CH3:2]

参加物

4

反応物 1

HCID 59152889(R)-[4-(3-isopropenyl-5-trifluoromethyl-benzenesulfonylamino)-4,5,6,7-tetrahydro-indazol-1-yl]-acetic acid ethyl ester

生成物 1

HCID 59152935(R)-[4-(3-isopropyl-5-trifluoromethyl-benzenesulfonylamino)-4,5,6,7-tetrahydro-indazol-1-yl]-acetic acid ethyl ester収率 96.8%

試薬・触媒・溶媒 2

HCID 23938Palladium触媒HCID 887Methanol溶媒

実験手順

A solution of (R)-[4-(3-isopropenyl-5-trifluoromethyl-benzenesulfonylamino)-4,5,6,7-tetrahydro-indazol-1-yl]-acetic acid ethyl ester (using a method analogous to the one described for 1st step intermediate of example 11-1) (34 mg, 0.072 mmol) in methanol was hydrogenated over 10% Pd/C (6 mg) under 30 psi for 3 hours at room temperature. The reaction mixture was filtered through a glass funnel and concentrated to afford (R)-[4-(3-isopropyl-5-trifluoromethyl-benzenesulfonylamino)-4,5,6,7-tetrahydro-indazol-1-yl]-acetic acid ethyl ester (33 mg, 96.8%) as a white solid. MS cald for C21H26F3N3O4S 473, obsd. (ESI+) [(M+H)+] 474.

後処理

  1. filtrationThe reaction mixture was filtered through a glass funnel
  2. concentrationconcentrated

出典と根拠

ORDレコード
ord-415dc4fab79548fb9b3c29dbbc1d74f6
出典データセット
uspto-grants-2012_02
特許番号
US08124641B2

反応ノート

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