関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Nicotinic Acid | HCID 938 | — |
| 反応物 | 4-Methylmorpholine | HCID 7972 | — |
| 反応物 | 1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride | HCID 2723939 | — |
| 反応物 | Amino-acetic acid 4-allyl-2-methoxy-phenyl ester | HCID 69920127 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | [(Pyridine-3-carbonyl)-amino]-acetic acid 4-allyl-2-methoxy-phenyl ester | HCID 53340886 | 43% |
反応手順
To a solution of Amino-acetic acid 4-allyl-2-methoxy-phenyl ester (510 mg, 1.7 mmol), in DCM (20 mL) were added niacin (0.23 g, 1.9 mmol), N-methyl morpholine (0.96 mL, 8.8 mmol), EDC.HCl (0.67 g, 3.5 mmol) at ice temperature (0° C.). The mixture was allowed to stir at room temperature (25° C.) over a period of 2 hrs. The resulting mixture was diluted with DCM (200 mL) washed with water (2×100 mL) and dried over sodium sulphate. The crude product obtained upon evaporation of the solvent was purified by silica gel column chromatography to obtain product as off-white solid (210 mg, 43%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US08846721B2 |
|---|
| 出典データセット | uspto-grants-2014_09 |
|---|
| ORD ID | ord-f7e798326e974114812ded31a5c65c31 |
|---|
| 出典メモ | uspto-grants-2014_09 |
|---|
