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1-(4-bromo-2-fluorophenyl)-1H-1,2,3,4-tetrazole → Tert-butyl 4-{5-[3-fluoro-4-(1H-tetrazol-1-yl)phenyl]benzo[d]oxazol-2-yl}piperidine-1-carboxylate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 1-(4-bromo-2-fluorophenyl)-1H-1,2,3,4-tetrazole | HCID 24695898 | — |
| 反応物 | Tert-butyl 4-(5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzo[d]oxazol-2-yl)piperidine-1-carboxylate | HCID 71090269 | — |
| 生成物 | Tert-butyl 4-{5-[3-fluoro-4-(1H-tetrazol-1-yl)phenyl]benzo[d]oxazol-2-yl}piperidine-1-carboxylate | HCID 71114205 | 20.6% |
反応手順
Following the General Procedure-3, the titled compound (22 mg) was prepared from Intermediate 8 (100 mg, 0.23 mmol) and 1-(4-bromo-2-fluorophenyl)-1H-tetrazole (56 mg, 0.23 mmol) as a pale-yellow solid. M.P.: 154-159° C. 1H-NMR (δ ppm, CDCl3, 400 MHz): 9.14 (d, J 2.5, 1H), 8.04 (t, J 7.8, 1H), 7.91 (d, J 3.9, 1H), 7.64-7.54 (m, 4H), 4.16 (d, J 10, 2H), 3.21-3.13 (m, 1H), 3.01 (t, J 11.9, 2H), 2.21-2.12 (m, 2H), 2.00-1.87 (m, 2H), 1.48 (s, 9H).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09181214B2 |
| 出典データセット | uspto-grants-2015_11 |
| ORD ID | ord-dcd684ab8bd64b8b87c79c66e449b79b |
| 出典メモ | uspto-grants-2015_11 |