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Triazabicyclodecene → 3-Amino-4-methyl-N-(2-(4-methylpiperazin-1-yl)benzyl)benzamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Triazabicyclodecene | HCID 79873 | — |
| 反応物 | Methyl 3-amino-4-methylbenzoate | HCID 337778 | — |
| 反応物 | 2-(4-Methyl-1-piperazinyl)benzenemethanamine | HCID 2795568 | — |
| 溶媒 | Toluene | HCID 1140 | — |
| 溶媒 | Ethyl Acetate | HCID 8857 | — |
| 生成物 | 3-Amino-4-methyl-N-(2-(4-methylpiperazin-1-yl)benzyl)benzamide | HCID 86695684 | — |
反応手順
A solution of methyl 3-amino-4-methylbenzoate (commercially available) (1.609 g, 9.74 mmol), TBD (2,3,4,6,7,8-hexahydro-1H-pyrimido[1,2-a]pyrimidine) (0.678 g, 4.87 mmol) and (2-(4-methylpiperazin-1-yl)phenyl)methanamine (commercially available) (2 g, 9.74 mmol) in toluene (30 ml) was heated at reflux overnight. The reaction mixture was diluted with EtOAc and washed with sat.NaHCO3 and water. The organic portion was separated, dried (MgSO4) and concentrated in vacuo. The product was purified by chromagraphy on silica eluting with a gradient of 0-20% 2M NH3 in MeOH/DCM to afford the title compound;
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08883819B2 |
| 出典データセット | uspto-grants-2014_11 |
| ORD ID | ord-71b9897385b34b5bb32f9468d007c604 |
| 出典メモ | uspto-grants-2014_11 |