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Thiophosgene → 4-(2-Amino-pyrimidin-5-yl)-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidine-7-carbothioic acid [4-(morpholine-4-carbonyl)-phenyl]-amide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Thiophosgene | HCID 10040 | — |
| 反応物 | 4-(Morpholine-4-carbonyl)aniline | HCID 577815 | — |
| 反応物 | Bis-(4-methoxybenzyl)-[5-(2-morpholin-4-yl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)-pyrimidin-2-yl]-amine | HCID 45258862 | — |
| 反応物 | 4-(4-Ethyl-piperazin-1-yl)-2,6-difluoro-phenylamine | HCID 59244379 | — |
| 生成物 | 4-(2-Amino-pyrimidin-5-yl)-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidine-7-carbothioic acid [4-(morpholine-4-carbonyl)-phenyl]-amide | HCID 59244491 | — |
反応手順
Using bis-(4-methoxy-benzyl)-[5-(2-morpholin-4-yl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)-pyrimidin-2-yl]-amine (80.9 mg) and (4-amino-phenyl)-morpholin-4-yl-methanone (37.1 mg) obtained in Step B in Example 1-D-104 instead of 4-(4-ethyl-piperazin-1-yl)-2,6-difluoro-phenylamine, and thiophosgene (22.9 μl) instead of triphosgene, in the same manner as Step D in Example 1-D-18, 4-{2-[bis-(4-methoxy-benzyl)-amino]-pyrimidin-5-yl}-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidine-7-carbothioic acid [4-(morpholine-4-carbonyl)-phenyl]-amide was obtained as a crude product. Further, in the same manner as Step D in Example 1-D-18, the desired compound (D-251) was obtained as a colorless solid (40.1 mg, 68%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08022205B2 |
| 出典データセット | uspto-grants-2011_09 |
| ORD ID | ord-359f82cf720f40e28e9ad49d9d55e593 |
| 出典メモ | uspto-grants-2011_09 |