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3,5-Difluorophenylacetic acid → 3[N'-(3,5-Difluorophenylacetyl)-L-alaninyl]amino-2,4-dioxo-1,5bis-(2-methylpropyl)-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 3,5-Difluorophenylacetic acid | HCID 145424 | — |
| 反応物 | 3-(L-alaninyl)amino-2,4-dioxo-1,5-bis-(2-methylpropyl)-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine hydrochloride | HCID 23552766 | — |
| 生成物 | 3[N'-(3,5-Difluorophenylacetyl)-L-alaninyl]amino-2,4-dioxo-1,5bis-(2-methylpropyl)-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine | HCID 22984081 | — |
反応手順
Following General Procedure I above using 3,5-difluorophenylacetic acid (Lancaster) and 3-(L-alaninyl)amino-2,4-dioxo-1,5-bis-(2-methylpropyl)-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine hydrochloride (Example 8-S), the title compound was prepared as a white solid (melting point=197-198° C.). Purification was by flash chromatography eluting with CH2Cl2/EtOAc (2:1 gradient to 3:4). Rf=0.23 (CH2Cl2/EtOAc, 1:1).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US06667305B1 |
| 出典データセット | uspto-grants-2003_12 |
| ORD ID | ord-300bd09ce1d94a9ba961a89718304931 |
| 出典メモ | uspto-grants-2003_12 |