関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Diethyl 2-(benzo[d]thiazol-2-yl)malonate | HCID 3922432 | — |
| 反応物 | Tert-butyl 4-carbamimidoylpiperidine-1-carboxylate | HCID 44828660 | — |
| 溶媒 | Toluene | HCID 1140 | — |
| 生成物 | HCID 178451809 | HCID 178451809 | 68.2% |
反応手順
A mixture of tert-butyl 4-carbamimidoylpiperidine-1-carboxylate (35 g, 153.98 mmol, 1.00 equiv) and 1,3-diethyl 2-(1,3-benzothiazol-2-yl)propanedioate (49.7 g, 169.43 mmol, 1.10 equiv) in toluene (500 ml) was heated overnight at 120° C. in an oil bath under nitrogen. After cooled to room temperature, the solid was collected by filtration. 45 g of tert-butyl 4-[5-(1,3-benzothiazol-2-yl)-4,6-dihydroxypyrimidin-2-yl]piperidine-1-carboxylate was obtained as a light yellow solid. MS m/z [M+H]+ (ESI): 429.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US09221809B2 |
|---|
| 出典データセット | uspto-grants-2015_12 |
|---|
| ORD ID | ord-a86ad43807cd4389ba07efb4203cdeb5 |
|---|
| 出典メモ | uspto-grants-2015_12 |
|---|
