関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Diethylamine | HCID 8021 | — |
| 反応物 | 1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride | HCID 2723939 | — |
| 反応物 | H-Orn(Z)-OH | HCID 7009570 | — |
| 反応物 | 5-(N-Boc-N-2-picolylaminomethyl)pyrazine-2-carboxylic Acid | HCID 21973652 | — |
| 触媒 | 4-(Dimethylamino)pyridine | HCID 14284 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | (5-(N-Boc-N-2-picolylaminomethyl)pyrazine-2-carbonyl)-Ndelta-Cbz-L-ornithine | HCID 86592263 | — |
反応手順
The compound obtained in Example 8-6 (160 mg) was dissolved in DMF (3.2 ml) and diethylamine (0.32 ml) was added. After one hour, the reaction solution was concebtrated and the residue obtained was dissolved in DMF (1 ml). Then, WSCI hydrochloride (73 mg), DMAP (31 mg), and a solution of the compound obtained in Example 13-3 in DMF (1 ml) were sequentially added. After 15 hours, the reaction solution was concentrated. After the addition of chloroform and 1 mol/l hydrochloric acid, the residue was extracted with chloroform. The organic layer was washed with saturated brine and dried over anhydrous sodium sulfate. The residue was crude-purified by silica gel column chromatography (4 g, chloroform/ethyl acetate=1/2) to obtain the title compound (95.2 mg) as colorless syrup.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07098215B2 |
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| 出典データセット | uspto-grants-2006_08 |
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| ORD ID | ord-27b3171f15d74f3eb8897b1eb4d4be90 |
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| 出典メモ | uspto-grants-2006_08 |
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