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Methoxyacetic Acid → N-[5-(4-Methanesulfonyl-3-trifluoromethyl-phenyl)-4-methyl-thiazol-2-yl]-2-methoxy-acetamide

HRID 1092989
ノート
印刷プレビュー

反応式

HRID 1092989 の反応式
[CH3:1][S:2]([C:5]1[CH:10]=[CH:9][C:8]([C:11]2[S:15][C:14]([NH2:16])=[N:13][C:12]=2[CH3:17])=[CH:7][C:6]=1[C:18]([F:21])([F:20])[F:19])(=[O:4])=[O:3].CN(C(ON1N=NC2C=CC=NC1=2)=[N+](C)C)C.F[P-](F)(F)(F)(F)F.[CH3:46][O:47][CH2:48][C:49](O)=[O:50].CCN(C(C)C)C(C)C>CN(C=O)C>[CH3:1][S:2]([C:5]1[CH:10]=[CH:9][C:8]([C:11]2[S:15][C:14]([NH:16][C:49](=[O:50])[CH2:48][O:47][CH3:46])=[N:13][C:12]=2[CH3:17])=[CH:7][C:6]=1[C:18]([F:21])([F:20])[F:19])(=[O:3])=[O:4]
参加物実験手順後処理出典と根拠反応ノート

参加物

6

反応物 4

HCID 12251Methoxyacetic AcidHCID 81531DiisopropylethylamineHCID 9886157Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)HCID 574737494-Methyl-5-(4-(methylsulfonyl)-3-(trifluoromethyl)phenyl)thiazol-2-amine

生成物 1

HCID 86598425N-[5-(4-Methanesulfonyl-3-trifluoromethyl-phenyl)-4-methyl-thiazol-2-yl]-2-methoxy-acetamide

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

5-(4-Methanesulfonyl-3-trifluoromethyl-phenyl)-4-methyl-thiazol-2-ylamine (158a) (0.1 g, 0.3 mmol) is added to a solution of HATU (0.226 g, 0.6 mmol), methoxyacetic acid (0.046 ml, 0.6 mmol) and DIPEA (0.1 ml, 0.6 mmol) in DMF (7.5 ml). The reaction mixture was left to stir for 3 days at room temperature. The reaction mixture is filtered through basic alumina. The solvent is removed in vacuo and the product is purified by chromatography on silica eluting with ethyl acetate-hexane (3:1) to give the titled compound.

後処理

  1. waitThe reaction mixture was left
  2. filtrationThe reaction mixture is filtered through basic alumina
  3. customThe solvent is removed in vacuo
  4. customthe product is purified by chromatography on silica eluting with ethyl acetate-hexane (3:1)

出典と根拠

ORDレコード
ord-613fbf8b1cef4e34a5da7e9ce1a2d44e
出典データセット
uspto-grants-2012_03
DOI
10.6084/m9.figshare.5104873.v1
特許番号
US08129541B2

反応ノート

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