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【结 构 式】 
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【分子编号】30419 【品名】3-amino-4-methoxybenzoic acid 【CA登记号】2840-26-8 |
【 分 子 式 】C8H9NO3 【 分 子 量 】167.1644 【元素组成】C 57.48% H 5.43% N 8.38% O 28.71% |
与该中间体有关的原料药合成路线共 1 条
合成路线1
该中间体在本合成路线中的序号：(I)8-Methoxyquinoline-5-carboxylic acid (III) was prepared by Skraup synthesis from 3-amino-4-methoxybenzoic acid (I) and glycerol (II) in sulfuric acid at 180 C. Subsequent treatment of (III) with oxalyl chloride using a catalytic amount of DMF gave the corresponding acid chloride (IV), which was finally coupled with 4-amino-3,5-dichloropyridine (V) in the presence of NaH in DMF to provide the target amide.
| 【1】 Buckley, G.M.; et al.; 8-Methoxyquinoline-5-carboxamides as PDE4 inhibitors: A potential treatment for asthma. Bioorg Med Chem Lett 2002, 12, 12, 1613. |
| 【2】 Dyke, H.J.; Montana, J.G.; Lowe, C.; Kendall, H.J.; Sabin, V.M. (Celltech Group plc); Quinoline carboxamides as TNF inhibitors and as PDE-IV inhibitors. EP 0952832; JP 2000510865; US 5804588; WO 9744036 . |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (I) | 30419 | 3-amino-4-methoxybenzoic acid | 2840-26-8 | C8H9NO3 | 详情 | 详情 |
| (II) | 13289 | Glycerine; Glycerin; Glycerol | 56-81-5 | C3H8O3 | 详情 | 详情 |
| (III) | 30420 | 8-methoxy-5-quinolinecarboxylic acid | C11H9NO3 | 详情 | 详情 | |
| (IV) | 30421 | 8-methoxy-5-quinolinecarbonyl chloride | C11H8ClNO2 | 详情 | 详情 | |
| (V) | 25135 | 3,5-dichloro-4-pyridinamine; 4-amino-3,5-dichloropyridine | 22889-78-7 | C5H4Cl2N2 | 详情 | 详情 |
Extended Information