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(Pyrimidin-5-yl)boronic acid → 6-(3-(2-Hydroxypropan-2-yl)azetidin-1-yl)-5-(pyrimidin-5-yl)-N-(4-(trifluoromethoxy)phenyl)nicotinamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | (Pyrimidin-5-yl)boronic acid | HCID 2795193 | — |
| 反応物 | 5-bromo-6-(3-(2-hydroxypropan-2-yl)azetidin-1-yl)-N-(4-(trifluoromethoxy)phenyl)nicotinamide | HCID 89907283 | — |
| 生成物 | 6-(3-(2-Hydroxypropan-2-yl)azetidin-1-yl)-5-(pyrimidin-5-yl)-N-(4-(trifluoromethoxy)phenyl)nicotinamide | HCID 89908451 | — |
反応手順
The title compound was prepared in an analogous fashion to that described in Example 128 using 5-bromo-6-(3-(2-hydroxypropan-2-yl)azetidin-1-yl)-N-(4-(trifluoromethoxy)phenyl)nicotinamide (Stage 142.1) and pyrimidin-5-ylboronic acid to afford an off-white powder. HPLC (Condition 4) tR=4.88 min, UPLC-MS (Condition 7) m/z=474.2 [M+H]+; 1H-NMR (400 MHz, DMSO-d6) δ ppm 0.94 (s, 6H) 2.50-2.58 (m, 1H) 3.63 (d, J=7.43 Hz, 4H) 4.39 (s, 1H) 7.34 (d, J=8.99 Hz, 2H) 7.49-7.68 (m, 1H) 7.79-7.91 (m, 2H) 8.06 (dd, J=2.15, 0.98 Hz, 1H) 8.73-8.81 (m, 1H) 8.85-8.96 (m, 1H) 9.20 (d, J=0.78 Hz, 1H) 10.19 (s, 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-07081c946dc9458a92d91c086c78f8fa |
| 出典メモ | uspto-grants-2016_03 |