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Ethyl 4-hydroxy-2-(methylsulfanyl)-5-pyrimidinecarboxylate → Ethyl 6-oxo-2-(((tetrahydrofuran-2-yl)methyl)amino)-1,6-dihydropyrimidine-5-carboxylate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Ethyl 4-hydroxy-2-(methylsulfanyl)-5-pyrimidinecarboxylate | HCID 239049 | — |
| 反応物 | Tetrahydrofurfurylamine | HCID 253298 | — |
| 溶媒 | Methanol | HCID 887 | — |
| 生成物 | Ethyl 6-oxo-2-(((tetrahydrofuran-2-yl)methyl)amino)-1,6-dihydropyrimidine-5-carboxylate | HCID 17229209 | 47% |
反応手順
(tetrahydrofuran-2-yl)methanamine (142 mg, 1.40 mmol) was added into ethyl 2-(methylthio)-6-oxo-1,6-dihydropyrmidine-5-carboxylate (300 mg, 1.40 mmol) in methanol and refluxed overnight. After half of the starting material was consumed, the reaction mixture was reheated again overnight. Then the reaction mixture was cooled and the precipitate filtered. 1H-NMR confirmed the product as ethyl 6-oxo-2-(((tetrahydrofuran-2-yl)methyl)amino)-1,6-dihydropyrimidine-5-carboxylate (HGN-0017) (176 mg, 47% yield).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09309232B2 |
| 出典データセット | uspto-grants-2016_04 |
| ORD ID | ord-48636987876e47b1832aee1079518157 |
| 出典メモ | uspto-grants-2016_04 |