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Dimethyl Ether → (3R)-4-Amino-3-[4-chloro-3-(3-hydroxyphenyl)phenyl]butanoic acid hydrochloride
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Dimethyl Ether | HCID 8254 | — |
| 反応物 | (3-Methoxyphenyl)boronic acid | HCID 2734370 | — |
| 反応物 | (4R)-4-(3-bromo-4-chlorophenyl)pyrrolidin-2-one | HCID 66724952 | — |
| 生成物 | (3R)-4-Amino-3-[4-chloro-3-(3-hydroxyphenyl)phenyl]butanoic acid hydrochloride | HCID 66724800 | — |
反応手順
Following the cross-coupling procedure according to Example 25 using 3-methoxyphenyl boronic acid and (4R)-4-(3-bromo-4-chlorophenyl)pyrrolidin-2-one followed by hydrolysis of the methyl ether using 48% HBr provided the title compound (34). 1H-NMR (400 MHz, CD3OD): δ 2.67-2.73 (dd, J=16.4, 6.4 Hz, 1H), 2.80-2.85 (dd, J=16.4, 7.6 Hz, 1H), 3.19-3.25 (dd, J=12.4, 12.0 Hz, 1H), 3.32-3.37 (m, 1H), 3.39-3.47 (m, 1H), 6.79-6.81 (m, 1H), 6.85-6.87 (m, 2H), 7.21-7.25 (m, 1H), 7.28-7.33 (m, 2H), 7.48-7.50 (d, J=8 Hz, 1H); MS (ESI) m/z 306.14 (M+H)+.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08344028B2 |
| 出典データセット | uspto-grants-2013_01 |
| ORD ID | ord-68b95ea487a34606981b7e29fa184205 |
| 出典メモ | uspto-grants-2013_01 |