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2-Chlorobenzaldehyde → Phthalimidoamlodipine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 2-Chlorobenzaldehyde | HCID 6996 | — |
| 反応物 | Methyl 3-aminocrotonate | HCID 643918 | — |
| 反応物 | Ethyl 4-(2-(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)ethoxy)-3-oxobutanoate | HCID 9840027 | — |
| 溶媒 | Isopropanol | HCID 3776 | — |
| 生成物 | Phthalimidoamlodipine | HCID 9871958 | — |
反応手順
Methyl 3-aminocrotonate (72.2 g; 0.627M) and 2-chlorobenzaldehyde (88.1 g; 0.627M) were added to a solution of ethyl 4-(2-phthalimidoethoxy)acetoacetate (200 g; 0.627M) in isopropanol (1 liter) and the mixture was heated under reflux for 20 hours. The isopropanol was evaporated under reduced pressure and replaced by acetic acid (1 liter). After granulation at 10° the solid was collected and slurried in methanol (300 ml). The solid was collected by filtration and dried in vacuo at 50° to afford the title compound, yield 84.4 g, m.p. 146°-147°.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US04661485 |
| 出典データセット | uspto-grants-1987_04 |
| ORD ID | ord-6367f97d732147bb82f221d710bc467d |
| 出典メモ | uspto-grants-1987_04 |