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Triethylamine → tert-Butyl 4-((6-(5-cyano-6-methoxypyrazin-2-ylamino)pyrimidin-4-ylamino)methyl)piperidine-1-carboxylate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | 1-Boc-4-(aminomethyl)piperidine | HCID 736817 | — |
| 反応物 | 5-(6-Chloropyrimidin-4-ylamino)-3-methoxypyrazine-2-carbonitrile | HCID 59613517 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 生成物 | tert-Butyl 4-((6-(5-cyano-6-methoxypyrazin-2-ylamino)pyrimidin-4-ylamino)methyl)piperidine-1-carboxylate | HCID 59613473 | 40.1% |
反応手順
A solution of 5-(6-chloropyrimidin-4-ylamino)-3-methoxypyrazine-2-carbonitrile (4.5 mg, 0.017 mmol), tert-butyl 4-(aminomethyl)piperidine-1-carboxylate (4 mg, 0.034 mmol) and triethylamine (12 uL, 0.085 mmol) in acetonitrile (1.5 mL) was heated at 145° C. for 90 min using microwave irradiation. The solvent was removed in vacuo and the crude mixture was purified by preparative thin layer chromatography, eluting with dichloromethane/MeOH (10/1), to give the title compound as a yellow oil (3 mg, 40%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08058045B2 |
| 出典データセット | uspto-grants-2011_11 |
| ORD ID | ord-1a8331d99ab64a759fd89feab08f57b7 |
| 出典メモ | uspto-grants-2011_11 |