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5-Fluoro-2-methylphenylboronic acid → N-(4-(Chlorodifluoromethoxy)phenyl)-6-((3S,4S)-3,4-dihydroxypyrrolidin-1-yl)-5-(5-fluoro-2-methylphenyl)nicotinamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 5-Fluoro-2-methylphenylboronic acid | HCID 2783190 | — |
| 反応物 | 5-Bromo-N-(4-(chlorodifluoromethoxy)phenyl)-6-((3S,4S)-3,4-dihydroxypyrrolidin-1-yl)nicotinamide | HCID 89906527 | — |
| 生成物 | N-(4-(Chlorodifluoromethoxy)phenyl)-6-((3S,4S)-3,4-dihydroxypyrrolidin-1-yl)-5-(5-fluoro-2-methylphenyl)nicotinamide | HCID 89908242 | — |
反応手順
The title compound was prepared in an analogous fashion to that described in Example 290 using 5-bromo-N-(4-(chlorodifluoromethoxy)phenyl)-6-((3S,4S)-3,4-dihydroxypyrrolidin-1-yl)nicotinamide (Stage 248.1) and 5-fluoro-2-methylphenylboronic acid to afford a white solid. HPLC (Condition 10) tR=6.25 min, UPLC-MS (Condition 11) tR=1.08 min, m/z=508.1 [M+H]+; 1H-NMR (400 MHz, DMSO-d6) δ ppm 1.59-1.90 (s, 2H) 1.95/2.06 (s, 3H) 2.76-3.00 (m, 1H) 3.04-3.25 (m, 2H) 4.09-4.21 (m, 1H) 4.76-4.90 (m, 2H) 7.08-7.17 (m, 1H) 7.25-7.35 (m, 4H) 7.81-7.97 (m, 3H) 8.74 (s, 1H) 10.07-10.17 (m, 1H).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09278981B2 |
| 出典データセット | uspto-grants-2016_03 |
| ORD ID | ord-48298f30a09142438374aafb15e1d690 |
| 出典メモ | uspto-grants-2016_03 |