4-(1,3-Oxazol-5-yl)benzenesulphonyl chloride → 4-Oxazol-5-yl-N-[4-(1-propyl-azetidin-3-yl)-phenyl]-benzenesulfonamide

HRID 1260245ノート

反応式

HRID 1260245 の反応式
[CH2:1]([N:4]1[CH2:7][CH:6]([C:8]2[CH:13]=[CH:12][C:11]([NH2:14])=[CH:10][CH:9]=2)[CH2:5]1)[CH2:2][CH3:3].[O:15]1[C:19]([C:20]2[CH:25]=[CH:24][C:23]([S:26](Cl)(=[O:28])=[O:27])=[CH:22][CH:21]=2)=[CH:18][N:17]=[CH:16]1>C(Cl)Cl.N1C=CC=CC=1.C(Cl)Cl>[O:15]1[C:19]([C:20]2[CH:21]=[CH:22][C:23]([S:26]([NH:14][C:11]3[CH:10]=[CH:9][C:8]([CH:6]4[CH2:5][N:4]([CH2:1][CH2:2][CH3:3])[CH2:7]4)=[CH:13][CH:12]=3)(=[O:28])=[O:27])=[CH:24][CH:25]=2)=[CH:18][N:17]=[CH:16]1

参加物

5

反応物 2

HCID 27764154-(1,3-Oxazol-5-yl)benzenesulphonyl chlorideHCID 57470084HCID 57470084、化合物

生成物 1

HCID 536286704-Oxazol-5-yl-N-[4-(1-propyl-azetidin-3-yl)-phenyl]-benzenesulfonamide収率 36%

試薬・触媒・溶媒 2

HCID 6344Dichloromethane溶媒HCID 21875418Pyridine methylene chloride溶媒

実験手順

The crude 4-(1-propyl-azetidin-3-yl)-phenylamine (40 mg, 0.21 mmol) was dissolved in CH2Cl2/pyridine 9:1 (10 ml) and 4-oxazol-5-yl-benzenesulfonyl chloride (51 mg, 0.21 mmol) was added. After stirring at room temperature for 2 h, the reaction mixture was diluted with CH2Cl2 and washed successively with 1N aqueous HCl, saturated aqueous NaHCO3 and water. The organic layer was dried over Na2SO4 and evaporated. The residue was chromatographied on silica gel (CH2Cl2:methanol, 95:5) to afford the title compound (30 mg, 36%) as a white amorphous solid.

後処理

  1. washwashed successively with 1N aqueous HCl, saturated aqueous NaHCO3 and water
  2. dry with materialThe organic layer was dried over Na2SO4
  3. customevaporated

出典と根拠

ORDレコード
ord-9e25afc090234df5a0cbcf25523bda15
出典データセット
uspto-grants-2013_06
特許番号
US08470810B2

反応ノート

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