Trifluoroacetic acid → 13-cyclohexyl-6-(1-cyclopropyl-4-(ethoxycarbonyl)-3-isopropyl-1H-pyrazol-5-yl)-3-methoxy-7H-indolo[2,1-a][2]benzazepine-10-carboxylic Acid

HRID 1094541ノート

反応式

HRID 1094541 の反応式
C(O)(C(F)(F)F)=O.[CH:8]1([C:14]2[C:15]3[CH:16]=[CH:17][C:18]([C:50]([O:52]C(C)(C)C)=[O:51])=[CH:19][C:20]=3[N:21]3[CH2:27][C:26]([C:28]4[N:32]([CH:33]5[CH2:35][CH2:34]5)[N:31]=[C:30]([CH:36]([CH3:38])[CH3:37])[C:29]=4[C:39]([O:41][CH2:42][CH3:43])=[O:40])=[CH:25][C:24]4[CH:44]=[C:45]([O:48][CH3:49])[CH:46]=[CH:47][C:23]=4[C:22]=23)[CH2:13][CH2:12][CH2:11][CH2:10][CH2:9]1>ClC(Cl)C>[CH:8]1([C:14]2[C:15]3[CH:16]=[CH:17][C:18]([C:50]([OH:52])=[O:51])=[CH:19][C:20]=3[N:21]3[CH2:27][C:26]([C:28]4[N:32]([CH:33]5[CH2:34][CH2:35]5)[N:31]=[C:30]([CH:36]([CH3:37])[CH3:38])[C:29]=4[C:39]([O:41][CH2:42][CH3:43])=[O:40])=[CH:25][C:24]4[CH:44]=[C:45]([O:48][CH3:49])[CH:46]=[CH:47][C:23]=4[C:22]=23)[CH2:9][CH2:10][CH2:11][CH2:12][CH2:13]1

参加物

4

反応物 2

HCID 6422Trifluoroacetic acidHCID 57953852tert-butyl 13-cyclohexyl-6-(1-cyclopropyl-4-(ethoxycarbonyl)-3-isopropyl-1H-pyrazol-5-yl)-3-methoxy-7H-indolo[2,1-a][2]benzazepine-10-carboxylate

生成物 1

HCID 5795385013-cyclohexyl-6-(1-cyclopropyl-4-(ethoxycarbonyl)-3-isopropyl-1H-pyrazol-5-yl)-3-methoxy-7H-indolo[2,1-a][2]benzazepine-10-carboxylic Acid収率 99.8%

試薬・触媒・溶媒 1

HCID 63651,1-Dichloroethane溶媒

実験手順

TFA (2.8 mL, 37 mmol) was added to a stirring solution of tert-butyl 13-cyclohexyl-6-(1-cyclopropyl-4-(ethoxycarbonyl)-3-isopropyl-1H-pyrazol-5-yl)-3-methoxy-7H-indolo[2,1-a][2]benzazepine-10-carboxylate (350 mg, 0.527 mmol) in dichloroethane (5 mL) at room temperature. The reaction was allowed to stir for 2.5 hrs and then was concentrated to dryness to give expected product (320 mg, 0.526 mmol, quant) consistent by LCMS.

後処理

  1. concentrationwas concentrated to dryness

出典と根拠

ORDレコード
ord-3b1c9a8aeaf84107a7587788f42db22d
出典データセット
uspto-grants-2012_03
特許番号
US08133884B2

反応ノート

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