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(2E)-3-(6-aminopyridin-3-yl)prop-2-enoic acid → (E)-3-(6-aminopyridin-3-yl)-N-(5-fluoro-1-methyl-1H-indol-3-ylmethyl)-N-methylacrylamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | (2E)-3-(6-aminopyridin-3-yl)prop-2-enoic acid | HCID 10487224 | — |
| 反応物 | 5-fluoro-1-methyl-3-(methylaminomethyl)-1H-indole | HCID 22139018 | — |
| 反応物 | 2,3-dihydro-8-(methylaminomethyl)-1H-3a-azacyclopenta[a]indene | HCID 22139048 | — |
| 反応物 | (E)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylic Acid Hydrochloride | HCID 66905305 | — |
| 生成物 | (E)-3-(6-aminopyridin-3-yl)-N-(5-fluoro-1-methyl-1H-indol-3-ylmethyl)-N-methylacrylamide | HCID 10337203 | 41% |
反応手順
According to the procedure of Example 24, except substituting 5-fluoro-1-methyl-3-(methylaminomethyl)-1H-indole (0.2 g, 1.04 mmole) for the 2,3-dihydro-8-(methylaminomethyl)-1H-3a-azacyclopenta[a]indene, and substituting (E)-3-(6-amino-pyridin-3-yl)acrylic acid (0.17 g, 1.04 mmole) for the (E)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylic acid hydrochloride salt, the title compound (0.14 g, 41%) was prepared as an off-white powder: MS (ES) m/e 339 (M+H)+.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07741339B2 |
| 出典データセット | uspto-grants-2010_06 |
| ORD ID | ord-5b22d1fcba864c72b2b5c571d3a625bf |
| 出典メモ | uspto-grants-2010_06 |