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【结 构 式】

【分子编号】52890

【品名】4-nitrophenyl 8-methoxy-2-(trifluoromethyl)-5-quinolinecarboxylate

【CA登记号】

【 分 子 式 】C18H11F3N2O5

【 分 子 量 】392.2910296

【元素组成】C 55.11% H 2.83% F 14.53% N 7.14% O 20.39%

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:(III)

8-Methoxy-2-trifluoromethylquinoline-5-carboxylic acid (I) was activated as the corresponding nitrophenyl ester (III) upon treatment with p-nitrophenol (II) and EDC. The p-nitrophenyl ester (III) was then coupled with 4-amino-3,5-dichloropyridine (IV) in the presence of NaH to produce amide (V). The pyridine ring of (V) was finally oxidized to the title N-oxide by treatment with peracetic acid.

1 Billah, M.; et al.; Synthesis and profile of SCH351591, a novel PDE4 inhibitor. Bioorg Med Chem Lett 2002, 12, 12, 1621.
2 Montana, J.G.; Dyke, H.J. (Celltech Group plc); N-Oxides of heterocyclic cpds. with TNF and PDE-IV inhibiting activity. EP 1045845; US 6262070; WO 0026208 .
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) 52889 8-methoxy-2-(trifluoromethyl)-5-quinolinecarboxylic acid C12H8F3NO3 详情 详情
(II) 11236 4-Nitrophenol; p-Nitrophenol 100-02-7 C6H5NO3 详情 详情
(III) 52890 4-nitrophenyl 8-methoxy-2-(trifluoromethyl)-5-quinolinecarboxylate C18H11F3N2O5 详情 详情
(IV) 25135 3,5-dichloro-4-pyridinamine; 4-amino-3,5-dichloropyridine 22889-78-7 C5H4Cl2N2 详情 详情
(V) 52891 N-(3,5-dichloro-4-pyridinyl)-8-methoxy-2-(trifluoromethyl)-5-quinolinecarboxamide C17H10Cl2F3N3O2 详情 详情
Extended Information