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Trifluoroacetic acid methylene chloride → (R)-1-(2-([1,2,4]triazolo[4,3-a]pyridin-3-yl)quinolin-8-yl)piperidin-3-amine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Trifluoroacetic acid methylene chloride | HCID 21863450 | — |
| 反応物 | (R)-tert-butyl 1-(2-([1,2,4]triazolo[4,3-a]pyridin-3-yl)quinolin-8-yl)piperidin-3-ylcarbamate | HCID 67234401 | — |
| 生成物 | (R)-1-(2-([1,2,4]triazolo[4,3-a]pyridin-3-yl)quinolin-8-yl)piperidin-3-amine | HCID 58304331 | 43% |
反応手順
(R)-tert-butyl 1-(2-([1,2,4]triazolo[4,3-a]pyridin-3-yl)quinolin-8-yl)piperidin-3-ylcarbamate (0.030 g, 0.067 mmol) was added to a 1:1 TFA-DCM and stirred for about 2 hours, at which time the reaction appeared complete by LC/TLC. The crude mixture was evaporated and purified by flash column chromatography (Horizon, using a gradient elution of 5% NH4 in MeOH/DCM). The desired product was isolated as a light yellow solid (10 mg; 43% yield). MS ESI (+) m/z 345.2 (M+1) detected.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08895550B2 |
| 出典データセット | uspto-grants-2014_11 |
| ORD ID | ord-09ac4f5e9a76466e94b01e148a408f63 |
| 出典メモ | uspto-grants-2014_11 |