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(4-(N-Isopropylsulfamoyl)phenyl)boronic acid → 1-Methylethyl 4-{[(4'-{[(1-methylethyl)amino]sulfonyl}-4-biphenylyl)oxy]methyl}-1-piperidinecarboxylate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | (4-(N-Isopropylsulfamoyl)phenyl)boronic acid | HCID 44119552 | — |
| 反応物 | 4-(4-Bromophenoxymethyl)piperidine-1-carboxylic acid isopropyl ester | HCID 57930300 | — |
| 生成物 | 1-Methylethyl 4-{[(4'-{[(1-methylethyl)amino]sulfonyl}-4-biphenylyl)oxy]methyl}-1-piperidinecarboxylate | HCID 59177769 | 9.9% |
反応手順
The title compound (9.4 mg, 8%) was prepared from (4-{[(1-methylethyl)amino]sulfonyl}phenyl)boronic acid (49 mg, 0.2 mmol) and 1-methylethyl 4-{[(4-bromophenyl)oxy]methyl}-1-piperidinecarboxylate (prepared as in Example 9, Step 2, 71 mg, 0.2 mmol) in a manner similar to Example 21, Step 3, and worked up in a manner similar to Example 9, Step 3. 1H NMR (400 MHz, CDCl3): δ 7.89 (d, 2H, J=8.6 Hz), 7.66 (d, 2H, J=8.6 Hz), 7.54 (d, 2H, J=8.9 Hz), 6.98 (d, 2H, J=8.8 Hz), 4.97-4.87 (m, 1H), 4.28-4.18 (m, 2H), 3.85 (d, 2H, J=6.4 Hz), 3.58-3.45 (m, 1H), 2.84-2.74 (m, 2H), 2.05-1.95 (m, 1H), 1.90-1.80 (m, 2H), 1.37-1.27 (m, 3H), 1.25 (d, 6H, J=6.4 Hz), 1.11 (d, 6H, J=6.5 Hz); LRMS (ESI), m/z 475 (M+H).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08101634B2 |
| 出典データセット | uspto-grants-2012_01 |
| ORD ID | ord-7cdcff0f7408469c85a7e0d546e0a27a |
| 出典メモ | uspto-grants-2012_01 |