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M-Cresol → Nalpha-(5-(N-2-picolylaminomethyl)thiophene-2-carbonyl)-L-ornithine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | M-Cresol | HCID 342 | — |
| 反応物 | Trifluoroacetic acid | HCID 6422 | — |
| 反応物 | Thioanisole | HCID 7520 | — |
| 反応物 | Nalpha-(5-(N-Boc-N-2-picolylaminomethyl)thiophene-2-carbonyl)-Ndelta-Cbz-L-ornithine | HCID 86592265 | — |
| 生成物 | Nalpha-(5-(N-2-picolylaminomethyl)thiophene-2-carbonyl)-L-ornithine | HCID 86592264 | 53.3% |
反応手順
A mixed solution of trifluoroacetic acid (1.4 ml), thioanisole (0.36 ml), and m-cresol (0.32 ml) was added to the compound obtained in Example 14-3 (56.2 mg). After 1.5 hours, the reaction solution was concentrated. Methanol was added to the residue and the mixture was washed with hexane. The methanol layer was concentrated and the residue was crude-purified by silica gel column chromatography (3 g, chloroform/methanol/water=7/3/0.5) to obtain the title compound (18.2 mg) as colorless syrup.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07098215B2 |
| 出典データセット | uspto-grants-2006_08 |
| ORD ID | ord-f1bdec720c284c5a909cb7ee228ab562 |
| 出典メモ | uspto-grants-2006_08 |