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

HRID 1260245노트

반응식

HRID 1260245 반응식
[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

참가 물질

5

반응물 2

HCID 27764154-(1,3-Oxazol-5-yl)benzenesulphonyl chlorideHCID 57470084HCID 57470084, 화합물

생성물 1

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

시약·촉매·용매 2

HCID 6344Dichloromethane용매HCID 21875418Pyridine methylene chloride용매

실험 절차

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.

후처리

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

출처 및 근거

ORD 기록
ord-9e25afc090234df5a0cbcf25523bda15
출처 데이터셋
uspto-grants-2013_06
특허 번호
US08470810B2

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