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HRID 229109作成日:2026年10月27日
Methyl Acetate → (r)-2-(3-{3-[[3-(Trifluoromethyl)-4-fluoro-benzyl](2,2-diphenylethyl)amino]-1-methyl-propoxy}-phenyl)acetic acid hydrochloride salt
https://huagongshe.com/reaction/229109
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Methyl Acetate | HCID 6584 | — |
| 反応物 | 4-Fluoro-3-(trifluoromethyl)benzaldehyde | HCID 522269 | — |
| 反応物 | 2-Chloro-3-(trifluoromethyl)benzaldehyde | HCID 2736672 | — |
| 反応物 | Ether hydrochloride | HCID 10953452 | — |
| 反応物 | (R)-2-(3-{3-[(2,2-diphenylethyl)amino]-1-methyl-propoxy}phenyl)acetic acid | HCID 68864815 | — |
| 溶媒 | Diethyl Ether | HCID 3283 | — |
| 生成物 | (r)-2-(3-{3-[[3-(Trifluoromethyl)-4-fluoro-benzyl](2,2-diphenylethyl)amino]-1-methyl-propoxy}-phenyl)acetic acid hydrochloride salt | HCID 68864196 | — |
反応手順
Following the procedure of Example 7(d) except (R)-2-(3-{3-[(2,2-diphenylethyl)amino]-1-methyl-propoxy}-phenyl)acetic acid and 3-(trifluoromethyl)-4-fluoro-benzaldehyde were used instead of (R)-2-(3-{3-(2,2-diphenylethyl)amino]-3-methyl-propoxy}phenyl)acetic acid methyl ester and 2-chloro-3-trifluoromethylbenzaldehyde in step (d) the corresponding carboxylic acid was obtained. The crude product was purified by preparative HPLC (TMC CombiPrep PDS, 75×30 mm, 25 mL/min, acetonitrile: H2O, UV detection at 254 nm) to afford the free base. The resulting amine/carboxylic acid was dissolved in Et2O (diethylether) and acidified with 1.0 M HCl/Et2O. The reaction mixture was concentrated in vacuo and dried under reduced pressure to give the title compound as a white solid, 95 mg (88%). MS (ESI) 580.6 (M+H+).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07560586B2 |
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| 出典データセット | uspto-grants-2009_07 |
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| ORD ID | ord-04f1056c8c994635b795ee80ded4a5ce |
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| 出典メモ | uspto-grants-2009_07 |
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