関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 4,6-Dichloropyrimidine | HCID 70943 | — |
| 反応物 | Lithium Hexamethyldisilazide | HCID 2733832 | — |
| 反応物 | 2-(Di-tert-butylphosphino)biphenyl | HCID 2734215 | — |
| 反応物 | 5-Amino-3-methoxypyrazine-2-carbonitrile | HCID 59613384 | — |
| 触媒 | Bis(dibenzylideneacetone)palladium | HCID 9811564 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 生成物 | 5-(6-Chloropyrimidin-4-ylamino)-3-methoxypyrazine-2-carbonitrile | HCID 59613517 | 28.1% |
反応手順
5-Amino-3-methoxypyrazine-2-carbonitrile (9.2 mg, 0.061 mmol), 4,6-dichloropyrimidine (10 mg, 0.067 mmol), lithium bis(trimethylsilyl)amide (1M, 75 uL, 0.075 mmol), Pd2(dba)3 (3.5 mg, 5.5% mol) and 2-(di-tert-butyl-phosphino)biphenyl (2 mg, 0.0067 mmol) were mixed in THF (0.5 mL). The reaction mixture was heated at 135° C. for 60 minutes using microwave irradiation. The crude product was purified by preparative thin layer chromatography, eluting with EtOAc/n-hexane (1/2), to give the title compound as an oil (4.5 mg, 28%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US08367658B2 |
|---|
| 出典データセット | uspto-grants-2013_02 |
|---|
| ORD ID | ord-6ad27cdb67e54f339e967b522c0fa9aa |
|---|
| 出典メモ | uspto-grants-2013_02 |
|---|
