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3-(Aminosulphonyl)benzeneboronic acid → N-(1-(6-amino-3-(3-sulfamoylphenyl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2-(5-fluoro-1H-indol-3-yl)acetamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 3-(Aminosulphonyl)benzeneboronic acid | HCID 44119323 | — |
| 反応物 | N-(1-(6-amino-3-bromopyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2-(5-fluoro-1H-indol-3-yl)acetamide | HCID 90281232 | — |
| 反応物 | (S)-5-(6-amino-2-(2-(3,5-difluorophenyl)-1-(2-(5-fluoro-1H-indol-3-yl)acetamido)ethyl)pyridin-3-yl)-2-fluorobenzamide | HCID 90281459 | — |
| 生成物 | N-(1-(6-amino-3-(3-sulfamoylphenyl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2-(5-fluoro-1H-indol-3-yl)acetamide | HCID 90281274 | — |
反応手順
The title compound was prepared according to the method presented for the synthesis of compound 1H of Example 1 utilizing 1G and (3-sulfamoylphenyl)boronic acid. 1H NMR (400 MHz, CDCl3) δ 8.15 (s, 1H), 8.03 (d, J=7.7 Hz, 1H), 7.96 (s, 2H), 7.91 (m, 1H), 7.57 (m, 3H), 7.24 (m, 1H), 6.92 (d, J=9.3 Hz, 2H), 6.70 (d, J=8.7 Hz, 1H), 6.54 (s, 1H), 6.20 (d, J=5.7 Hz, 2H), 5.54 (s, 2H), 5.33 (d, J=9.0 Hz, 1H), 3.63 (s, 2H), 2.99-2.85 (m, 2H). MS (m/z) 580.0 [M+H]+.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09050344B2 |
| 出典データセット | uspto-grants-2015_06 |
| ORD ID | ord-a24eb354086c4364a46c743ddb31bd73 |
| 出典メモ | uspto-grants-2015_06 |