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Diethyl cyanophosphonate → n-(4-(5-((Benzyl(methyl)amino)methyl)-1-(2,6-difluorobenzyl)-3-(4-(1-hydroxy-1-methylethyl)phenyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-n'-methoxyurea
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Diethyl cyanophosphonate | HCID 76257 | — |
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | Sodium ethoxide | HCID 2723922 | — |
| 反応物 | 2-(4-Aminophenyl)propan-2-ol | HCID 9543261 | — |
| 反応物 | 4-((Benzyl(methyl)amino)methyl)-2-((2,6-difluorobenzyl)(ethoxycarbonyl)amino)-5-(4-(3-methoxyureido)phenyl)thiophene-3-carboxylic acid | HCID 18324800 | — |
| 溶媒 | Ethanol | HCID 702 | — |
| 生成物 | n-(4-(5-((Benzyl(methyl)amino)methyl)-1-(2,6-difluorobenzyl)-3-(4-(1-hydroxy-1-methylethyl)phenyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-n'-methoxyurea | HCID 59000902 | 21.2% |
反応手順
The similar reaction as described in Example 40 by using 4-(N-benzyl-N-methylaminomethyl)-2-[N-(2,6-difluorobenzyl)-N-ethoxycarbonylamino]-5-[4-(3-methoxyureido)phenyl]thiophene-3-carboxylic acid (470 mg), diethyl cyanophosphate (167 μl), 4-(1-hydroxy-1-methylethyl)aniline (166 mg) and N-ethyldiisopropylamine (209 μl) gave a crude amide (422 mg). Furthermore, the similar reaction by using ethanol (25.5 ml) and sodium ethoxide (70 mg) gave the title compound (113 mg).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08058280B2 |
| 出典データセット | uspto-grants-2011_11 |
| ORD ID | ord-2871feba48bc496b84b7b62d843d8189 |
| 出典メモ | uspto-grants-2011_11 |