化工社化工社 化学情報印刷レポート · 研究参考用
HRID 2090322作成日：2026年10月27日
4-Cyanopiperidine → 1-{2-[2-Amino-6-(4-methylpiperazin-1-yl)pyrimidin-4-yl]-1,2,3,4-tetrahydroisoquinolin-7-yl}piperidine-4-carbonitrile
https://huagongshe.com/reaction/2090322
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 4-Cyanopiperidine | HCID 138223 | — |
| 反応物 | Sodium t-butoxide | HCID 23676156 | — |
| 反応物 | 4-(7-bromo-3,4-dihydroisoquinolin-2(1H)-yl)-6-(4-methylpiperazin-1-yl)pyrimidin-2-amine | HCID 46701048 | — |
| 触媒 | 2-(2'-Di-tert-butylphosphine)biphenylpalladium(II) acetate | HCID 11982262 | — |
| 生成物 | 1-{2-[2-Amino-6-(4-methylpiperazin-1-yl)pyrimidin-4-yl]-1,2,3,4-tetrahydroisoquinolin-7-yl}piperidine-4-carbonitrile | HCID 46701462 | — |
反応手順
A mixture of 4-(7-bromo-3,4-dihydroisoquinolin-2(1H)-yl)-6-(4-methylpiperazin-1-yl)pyrimidin-2-amine (40 mg, 0.1 mmol), piperidine-4-carbonitrile (22 mg, 0.20 mmol, Oakwood, Cat. No. 024547), sodium tert-butoxide (23 mg, 0.24 mmol), 2-(2′-di-tert-butylphosphine)biphenyl palladium(II) acetate (2.8 mg, 0.0060 mmol, Aldrich, Cat. No. 655414) in 1,4-dioxane (1 mL) was degassed with nitrogen and then heated at 120° C. overnight. The reaction mixture was cooled to r.t. and concentrated under reduced pressure. The residue was dissolved in MeOH and purified by RP-HPLC (pH=10) to afford the desired compound. LCMS (M+H)+: m/z=433.3.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US08436008B2 |
|---|
| 出典データセット | uspto-grants-2013_05 |
|---|
| ORD ID | ord-7d41bb556b24467fb5db54ab3a41d640 |
|---|
| 出典メモ | uspto-grants-2013_05 |
|---|
