関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Methylamine | HCID 6329 | — |
| 反応物 | (1S,3S)-1-(1,3-Benzodioxol-5-yl)-2-(2-chloroacetyl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylic Acid Methyl Ester | HCID 68502869 | — |
| 溶媒 | Methanol | HCID 887 | — |
| 生成物 | Tadalafil | HCID 110635 | — |
反応手順
Cis-1 -benzo [1,3 ]dioxol-5 -yl-2-(2-chloro-acetyl)-2,3,4,9-tetrahydro-1H-beta-carboline-3-carboxylic acid methyl ester (30 g) was taken in methanol (450 ml). The resultant mixture was heated to 35-40° C. and aqueous methyl amine (27 ml; 40%) was added. The reaction mixture was stirred at 50-55° C. for 5 hours and then cooled to 10-15° C. with continuous stirring for 0.5 hours. The solid so obtained was filtered and dried to afford (6R,12aR) 6-(1,3-benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methylpyrazino [1′,2′:1,6] pyrido[3,4-b]indole-1,4-dione.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US08445698B2 |
|---|
| 出典データセット | uspto-grants-2013_05 |
|---|
| ORD ID | ord-94c1d194673c4f0caf639c2655e57a4d |
|---|
| 出典メモ | uspto-grants-2013_05 |
|---|
