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2-Aminothiazole → 2-(4-Cyclopropanesulfonylphenyl)-2-(2,4-difluoro-phenoxy)-N-thiazol-2-yl-acetamide

HRID 1889190
ノート
印刷プレビュー

反応式

HRID 1889190 の反応式
[CH:1]1([S:4]([C:7]2[CH:12]=[CH:11][C:10]([CH:13]([O:17][C:18]3[CH:23]=[CH:22][C:21]([F:24])=[CH:20][C:19]=3[F:25])[C:14](O)=[O:15])=[CH:9][CH:8]=2)(=[O:6])=[O:5])[CH2:3][CH2:2]1.[NH2:26][C:27]1[S:28][CH:29]=[CH:30][N:31]=1.C1C=CC2N(O)N=NC=2C=1.CCN=C=NCCCN(C)C>C(Cl)Cl.O.C(N(CC)CC)C>[CH:1]1([S:4]([C:7]2[CH:12]=[CH:11][C:10]([CH:13]([O:17][C:18]3[CH:23]=[CH:22][C:21]([F:24])=[CH:20][C:19]=3[F:25])[C:14]([NH:26][C:27]3[S:28][CH:29]=[CH:30][N:31]=3)=[O:15])=[CH:9][CH:8]=2)(=[O:6])=[O:5])[CH2:2][CH2:3]1
参加物実験手順後処理出典と根拠反応ノート

参加物

8

反応物 4

HCID 21552-AminothiazoleHCID 159081-Ethyl-3-(3'-dimethylaminopropyl)carbodiimideHCID 757711-HydroxybenzotriazoleHCID 596100322-(4-Cyclopropylsulfonylphenyl)-2-(2,4-difluorophenoxy)acetic acid

生成物 1

HCID 252619862-(4-Cyclopropanesulfonylphenyl)-2-(2,4-difluoro-phenoxy)-N-thiazol-2-yl-acetamide

試薬・触媒・溶媒 3

HCID 962
Water
溶媒
HCID 6344Dichloromethane溶媒2 回
HCID 8471Triethylamine溶媒

実験手順

Procedure-A: To a mixture of 2-(4-cyclopropanesulfonylphenyl)-2-(2,4-difluorophenoxy)acetic acid (obtained in step III), 2-aminothiazole, HOBt, and EDCI, in methylene chloride, was added triethyl amine. The resulting mixture was stirred at room temperature overnight followed by dilution with methylene chloride. The reaction mixture was poured into water; organic layer was washed with water, brine, dried over sodium sulfate, and the organic solvent evaporated to get a residue which was purified by preparative TLC or column chromatoghaphy to provide the title compound.

後処理

  1. washorganic layer was washed with water, brine
  2. dry with materialdried over sodium sulfate
  3. customthe organic solvent evaporated
  4. customto get a residue which
  5. customwas purified by preparative TLC or column chromatoghaphy

出典と根拠

ORDレコード
ord-959577735b364c9ba5b181a161f104ca
出典データセット
uspto-grants-2013_08
DOI
10.6084/m9.figshare.5104873.v1
特許番号
US08501955B2

反応ノート

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