Potassium Carbonate → 2-Chloro-5-((2,2-difluorocyclopropyl)methoxy)pyrimidine
反応式
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]=1参加物
5
反応条件
- 温度
- 80 °C
実験手順
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).
後処理
- 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)
出典と根拠
- ORDレコード
- ord-f95e53fa1e424eae8b0b244b95016dec
- 出典データセット
- uspto-grants-2013_09
- 特許番号
- US08530460B2
反応ノート
読み込み中…