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Dopac → 2-Amino-4-[1-(3,4-dihydroxyphenylacetyl)-4-piperidinyl]quinazoline
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Dopac | HCID 547 | — |
| 反応物 | 2-Amino-4-(4-piperidinyl)quinazoline | HCID 15428775 | — |
| 触媒 | 4-(Dimethylamino)pyridine | HCID 14284 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | 2-Amino-4-[1-(3,4-dihydroxyphenylacetyl)-4-piperidinyl]quinazoline | HCID 21851548 | 60.2% |
反応手順
To an ice-cold solution of 2-amino-4-(4-piperidinyl)quinazoline (600 mg, 2.63 mmol) obtained in example 11(1), 3,4-dihydroxyphenylacetic acid (530 mg, 3.16 mmol) and 4-dimethylaminopyridine (386 mg, 3.16 mmol) in dimethylformamide (20 ml) was added 1-ethyl-3-(N,N'-dimethylaminopropyl)carbodiimide hydrochloride (605 mg, 3.16 mmol) under a nitrogen atmosphere. The mixture was stirred overnight at room temperature. The solvent was removed in vacuo and the residue was crystallized from methanol to give the titled compound (599 mg).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US05948786 |
| 出典データセット | uspto-grants-1999_09 |
| ORD ID | ord-1a25b87a62d743c3ad64eaa5fa0c8dcd |
| 出典メモ | uspto-grants-1999_09 |