Morpholine → 4-(5-Bromopyrimidin-2-yl)morpholine

HRID 734347

반응식

HRID 734347 반응식
C(=O)([O-])[O-].[K+].[K+].Cl[C:8]1[N:13]=[CH:12][C:11]([Br:14])=[CH:10][N:9]=1.[NH:15]1[CH2:20][CH2:19][O:18][CH2:17][CH2:16]1>CN(C=O)C>[Br:14][C:11]1[CH:10]=[N:9][C:8]([N:15]2[CH2:20][CH2:19][O:18][CH2:17][CH2:16]2)=[N:13][CH:12]=1

참가 물질

5

반응물 3

HCID 8083MorpholineHCID 11430Potassium CarbonateHCID 6066655-Bromo-2-chloropyrimidine

생성물 1

HCID 51443624-(5-Bromopyrimidin-2-yl)morpholine수율 35.7%

시약·촉매·용매 1

HCID 6228Dimethylformamide용매

실험 절차

Potassium carbonate (0.34 g) was added to a solution of 2-chloro-5-bromo-pyrimidine (0.5 g) in DMF (20 ml). The reaction mixture was stirred at rt for 15 min. Morpholine (0.2 g) was added and the reaction mixture was stirred at rt for 2 h. The excess DMF was removed by evaporation and the residue was partitioned between H2O/EtOAc (30:30 ml) The EtOAc layer was dried (MgSO4) and evaporated to dryness to give the sub-title compound as a cream solid (0.2 g). LCMS electrospray(+ve) 246 (MH+).

후처리

  1. stirringthe reaction mixture was stirred at rt for 2 h
  2. customThe excess DMF was removed by evaporation
  3. customthe residue was partitioned between H2O/EtOAc (30:30 ml) The EtOAc layer
  4. dry with materialwas dried (MgSO4)
  5. customevaporated to dryness

출처 및 근거

ORD 기록
ord-ab2a6236d2154eccafc76ab11566ee69
출처 데이터셋
uspto-grants-2009_09
특허 번호
US07592347B2

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