関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Trifluoroacetic acid | HCID 6422 | — |
| 反応物 | Pentamethylbenzene | HCID 12784 | — |
| 反応物 | methyl (1S)-1-{[(1S)-1-(4-methoxyphenyl)ethyl]amino}indane-5-carboxylate | HCID 86713454 | — |
| 生成物 | (S)-methyl 1-amino-2,3-dihydro-1H-indene-5-carboxylate | HCID 59460662 | 62.1% |
反応手順
To 452 mg of methyl (1S)-1-{[(1S)-1-(4-methoxyphenyl)ethyl]amino}indane-5-carboxylate were added 34 ml of trifluoroacetic acid and 1.03 g of pentamethylbenzene, followed by stirring at 70° C. for 4 days, and the solvent was evaporated under reduced pressure. To the obtained residue were added a saturated aqueous sodium hydrogen carbonate solution and chloroform to carry out a layer separation operation. The organic layer was washed with saturated brine and dried over anhydrous magnesium sulfate, and the solvent was evaporated under reduced pressure. The obtained residue was purified by silica gel column chromatography to obtain 165 mg of methyl (1S)-1-aminoindane-5-carboxylate.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US09447090B2 |
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| 出典データセット | uspto-grants-2016_09 |
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| ORD ID | ord-7346f4a4800a40d8af71c4b993c44102 |
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| 出典メモ | uspto-grants-2016_09 |
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