Potassium Carbonate → 2-Chloro-5-((2,2-difluorocyclopropyl)methoxy)pyrimidine
반응식
Br[CH2:2][CH:3]1[CH2:5][C:4]1([F:7])[F:6].C([O-])([O-])=O.[K+].[K+].[Cl:14][C:15]1[N:20]=[CH:19][C:18]([OH:21])=[CH:17][N:16]=1>CN(C=O)C>[Cl:14][C:15]1[N:20]=[CH:19][C:18]([O:21][CH2:2][CH:3]2[CH2:5][C:4]2([F:7])[F:6])=[CH:17][N:16]=1참가 물질
5
반응 조건
- 온도
- 80 °C
실험 절차
295 mg (1.72 mmol) 1-bromomethyl-2,2-difluorocyclopropane and 318 mg (2.30 mmol) K2CO3 are added to a mixture of 150 mg (1.15 mmol) 2-chloro-5-hydroxypyrimidine in 2 mL DMF. The mixture is stirred at 80° C. over night. Then the reaction mixture is quenched by the addition of water and extracted with DCM. The organic layer is dried with Na2SO4 and the solvent is removed in vacuo. The residue is purified by HPLC (MeOH/H2O/NH3).
후처리
- customThen the reaction mixture is quenched by the addition of water
- extractionextracted with DCM
- dry with materialThe organic layer is dried with Na2SO4
- customthe solvent is removed in vacuo
- customThe residue is purified by HPLC (MeOH/H2O/NH3)
출처 및 근거
- ORD 기록
- ord-f95e53fa1e424eae8b0b244b95016dec
- 출처 데이터셋
- uspto-grants-2013_09
- 특허 번호
- US08530460B2
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