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5-氨基吲唑 → 2-[4-(5-Chloro-2-cyanophenyl)-5-methoxy-2-oxopyridin-1(2H)-yl]-N-(1H-indazol-5-yl)-4-methoxybutanamide
参与物
| 角色 | 名称 | HCID | 投料 |
|---|---|---|---|
| 反应物 | 5-氨基吲唑 | HCID 88012 | — |
| 反应物 | 2-[4-(5-Chloro-2-cyanophenyl)-5-methoxy-2-oxopyridin-1(2H)-yl]-4-methoxybutanoic acid | HCID 117622944 | — |
| 产物 | 2-[4-(5-Chloro-2-cyanophenyl)-5-methoxy-2-oxopyridin-1(2H)-yl]-N-(1H-indazol-5-yl)-4-methoxybutanamide | HCID 117622784 | — |
反应步骤
150 mg (398 μmol) of 2-[4-(5-chloro-2-cyanophenyl)-5-methoxy-2-oxopyridin-1(2H)-yl]-4-methoxybutanoic acid (racemate) and 58.3 mg (438 μmol, 1.1 eq.) of 5-aminoindazole were reacted according to General Method 1. The crude product was purified by preparative HPLC (column: Chromatorex 125 mm×30 mm, 10 μm, mobile phase: water and acetonitrile, gradient 10% acetonitrile to 90% acetonitrile). Yield: 88 mg (42% of theory)
来源与证据
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 专利号 | US09434690B2 |
| 来源数据集 | uspto-grants-2016_09 |
| ORD ID | ord-9e53352ef2f2401390beafe919003b6d |
| 来源说明 | uspto-grants-2016_09 |