Pyrazole → HCID 68485174, 화합물

HRID 383289노트

반응식

HRID 383289 반응식
Cl[C:2]1[CH:7]=[C:6]([C:8]2[N:12]3[CH:13]=[C:14]([NH:17][CH:18]4[CH2:23][CH2:22][CH:21]([OH:24])[CH2:20][CH2:19]4)[CH:15]=[CH:16][C:11]3=[N:10][CH:9]=2)[CH:5]=[CH:4][N:3]=1.[NH:25]1[CH:29]=[CH:28][CH:27]=[N:26]1.C(=O)([O-])[O-].[Cs+].[Cs+]>CN(C=O)C>[N:25]1([C:2]2[CH:7]=[C:6]([C:8]3[N:12]4[CH:13]=[C:14]([NH:17][CH:18]5[CH2:23][CH2:22][CH:21]([OH:24])[CH2:20][CH2:19]5)[CH:15]=[CH:16][C:11]4=[N:10][CH:9]=3)[CH:5]=[CH:4][N:3]=2)[CH:29]=[CH:28][CH:27]=[N:26]1

참가 물질

5

반응물 3

HCID 1048PyrazoleHCID 10796Cesium carbonateHCID 252619024-[3-(2-Chloro-pyridin-4-yl)-imidazo[1,2-a]pyridin-6-ylamino]-cyclohexanol

생성물 1

HCID 68485174HCID 68485174, 화합물

시약·촉매·용매 1

HCID 6228Dimethylformamide용매

실험 절차

A mixture comprising [4-[3-(2-Chloro-pyridin-4-yl)-imidazo[1,2-a]pyridin-6-ylamino]-cyclohexanol (Example 2.1) (1 eq, 0.29 mmol, 100 mg), pyrazole (5 eq, 1.45 mmol, 99 mg) and cesium carbonate (3 eq, 0.87 mmol, 284 mg) in DMF (25 ml) is heated using microwave radiation at 145° C. for 6 hours. After cooling to room temperature, the mixture is loaded onto a SCX-2 cartridge eluting with MeOH followed by 2M NH3 in MeOH. The solvent is removed in vacuo and the crude product is triturated with ethyl acetate to afford the title compound; [M+H]+=375

후처리

  1. temperatureis heated
  2. customat 145° C.
  3. customfor 6 hours
  4. washeluting with MeOH
  5. customThe solvent is removed in vacuo
  6. customthe crude product is triturated with ethyl acetate

출처 및 근거

ORD 기록
ord-06cc73b89da14582ab5ac35f6b642553
출처 데이터셋
uspto-grants-2013_02
특허 번호
US08367662B2

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