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Potassium Carbonate → tert-Butyl {4-[5-(2,5-difluorophenoxy)-7-propoxyoxazolo[5,4-d]pyrimidin-2-yl]-2,6-dimethylphenoxy}acetate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | 2,5-Difluorophenol | HCID 94952 | — |
| 反応物 | Sodium Bisulfate | HCID 516919 | — |
| 反応物 | Tert-butyl [4-(5-methanesulfonyl-7-propoxyoxazolo[5,4-d]pyrimidin-2-yl)-2,6-dimethylphenoxy]acetate | HCID 86679896 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | tert-Butyl {4-[5-(2,5-difluorophenoxy)-7-propoxyoxazolo[5,4-d]pyrimidin-2-yl]-2,6-dimethylphenoxy}acetate | HCID 86679897 | 62.6% |
反応手順
To a solution of 100 mg [4-(5-methanesulfonyl-7-propoxy-oxazolo[5,4-d]pyrimidin-2-yl)-2,6-dimethyl-phenoxy]-acetic acid tert-butyl ester in 1.5 ml of N,N-dimethylformamide were added 62 mg of potassium carbonate and 32 mg of 2,5-difluoro-phenol. The mixture was stirred at room temperature for 12 h. Then the mixture was poured onto water, neutralized by addition of a 10% aqueous solution of sodium hydrogensulfate, and extracted twice with ethyl acetate. The combined organic layers were dried and concentrated in vacuo. After filtration the solvent was distilled off in vacuo and the residue purified by preparative HPLC to yield 69 mg of the title compound.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08748436B2 |
| 出典データセット | uspto-grants-2014_06 |
| ORD ID | ord-586565833103405e8359d34c96995918 |
| 出典メモ | uspto-grants-2014_06 |