Ethyl trifluoroacetate → 2,2,2-trifluoro-N-((1R,2S)-1-(1-(4-fluorophenyl)-1H-indazol-5-ylthio)-1-phenylpropan-2-yl)acetamide

HRID 13121

反応式

HRID 13121 の反応式
[F:1][C:2]1[CH:7]=[CH:6][C:5]([N:8]2[C:16]3[C:11](=[CH:12][C:13]([S:17][C@H:18]([C:22]4[CH:27]=[CH:26][CH:25]=[CH:24][CH:23]=4)[C@@H:19]([NH2:21])[CH3:20])=[CH:14][CH:15]=3)[CH:10]=[N:9]2)=[CH:4][CH:3]=1.CN(C)C(N(C)C)=N.[F:36][C:37]([F:44])([F:43])[C:38](OCC)=[O:39]>CO>[F:36][C:37]([F:44])([F:43])[C:38]([NH:21][C@@H:19]([CH3:20])[C@H:18]([S:17][C:13]1[CH:12]=[C:11]2[C:16](=[CH:15][CH:14]=1)[N:8]([C:5]1[CH:6]=[CH:7][C:2]([F:1])=[CH:3][CH:4]=1)[N:9]=[CH:10]2)[C:22]1[CH:23]=[CH:24][CH:25]=[CH:26][CH:27]=1)=[O:39]

参加物

5

反応物 3

HCID 9794Ethyl trifluoroacetateHCID 664601,1,3,3-TetramethylguanidineHCID 59339625(1R,2S)-1-(1-(4-fluorophenyl)-1H-indazol-5-ylthio)-1-phenylpropan-2-amine

生成物 1

HCID 593399122,2,2-trifluoro-N-((1R,2S)-1-(1-(4-fluorophenyl)-1H-indazol-5-ylthio)-1-phenylpropan-2-yl)acetamide収率 56.3%

試薬・触媒・溶媒 1

HCID 887Methanol溶媒

実験手順

To (1R,2S)-1-(1-(4-fluorophenyl)-1H-indazol-5-ylthio)-1-phenylpropan-2-amine (0.024 g, 0.06 mmol) in MeOH (2.5 mL), 1,1,3,3-tetramethylguanidine (0.056 mL, 0.45 mmol) and ethyl trifluoroacetate (0.114 mL, 0.95 mmol) was added and the mixture was stirred at rt O/N and than submitted to purification on HPLC. The relevant fractions were collected freezdried to give 16 mg of product (53% yield) which was analysed by LC/MS and NMR.

後処理

  1. customthan submitted to purification on HPLC
  2. customThe relevant fractions were collected freezdried

出典と根拠

ORDレコード
ord-f9e8e1eba8144cbf8b6781d2dd306d7c
出典データセット
uspto-grants-2010_06
特許番号
US07728030B2

関連ノート

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