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5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxylic Acid → 5-[5-(2,6-dichloro-phenylmethanesulfonyl)-2-oxo-1,2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxylic Acid | HCID 11073792 | — |
| 反応物 | 5-(2,6-Dichloro-phenylmethanesulfonyl)-1,3-dihydro-indol-2-one | HCID 18179768 | — |
| 生成物 | 5-[5-(2,6-dichloro-phenylmethanesulfonyl)-2-oxo-1,2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid | HCID 59077507 | — |
反応手順
5-(2,6-Dichloro-phenylmethanesulfonyl)-1,3-dihydro-indol-2-one was condensed with 5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxylic acid using the general condensation method to give 5-[5-(2,6-dichloro-phenylmethanesulfonyl)-2-oxo-1,2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid. This was then coupled with cyclopropyl-piperidin-4-yl-amine TFA salt (prepared as in lit. procedure by H. C. Hansen et al. Bioorg. Med. Chem. Lett. 10, 2000, 2435-2439.) using the general amidation procedure to give an orange solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US06599902B2 |
| 出典データセット | uspto-grants-2003_07 |
| ORD ID | ord-a951ae529f0a46549278182f652c6c0d |
| 出典メモ | uspto-grants-2003_07 |