|
【结 构 式】 
|
【药物名称】CI-1040, PD-184352 【化学名称】2-(2-Chloro-4-iodophenylamino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide 【CA登记号】212631-79-3 【 分 子 式 】C17H14ClF2IN2O2 【 分 子 量 】478.66753 |
【开发单位】Pfizer (Originator) 【药理作用】ONCOLYTIC DRUGS, Inhibitors of Signal Transduction Pathways, Mitogen-Activated Protein (MAP) Kinase Inhibitors |
合成路线1
The condensation of 2,3,4-trifluorobenzoic acid (I) with 2-chloro-4-iodoaniline (II) in the presence of LDA in THF afforded the aryl anthranilic acid (III), which was then coupled with O-(cyclopropylmethyl)hydroxylamine (IV) using bromo-tris(pyrrolidino)phosphonium hexafluorophosphate (PyBrOP) to furnish the title hydroxamate.
| 【1】 Tecle, H.; Dudley, D.T.; Bridges, A.J.; Barrett, S.D.; Saltiel, A.R.; Doherty, A.M. (Pfizer Inc.); 4-Bromo or 4-iodo phenylamino benzhydroxamic acid derivs. and their use as MEK inhibitors. EP 0993439; WO 9901426 . |
| 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) | 34622 | 2,3,4-trifluorobenzoic acid | 61079-72-9 | C7H3F3O2 | 详情 | 详情 |
| (II) | 34623 | 2-chloro-4-iodophenylamine; 2-chloro-4-iodoaniline | 42016-93-3 | C6H5ClIN | 详情 | 详情 |
| (III) | 34624 | 2-(2-chloro-4-iodoanilino)-3,4-difluorobenzoic acid | C13H7ClF2INO2 | 详情 | 详情 | |
| (IV) | 34625 | O-(cyclopropylmethyl)hydroxylamine; 1-[(aminooxy)methyl]cyclopropane | C4H9NO | 详情 | 详情 |
Extended Information