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【结 构 式】 
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【药物名称】D-24851 【化学名称】2-[1-(4-Chlorobenzyl)-1H-indol-3-yl]-2-oxo-N-(4-pyridyl)acetamide 【CA登记号】204205-90-3 【 分 子 式 】C22H16ClN3O2 【 分 子 量 】389.84472 |
【开发单位】Baxter Oncology (Originator) 【药理作用】Oncolytic Drugs, Solid Tumors Therapy, Antimitotic Drugs, Microtubule-Stabilizing Agents |
合成路线1
The condensation of 1H-indole (I) with 4-chlorobenzyl chloride (II) by means of NaH in DMSO gives 1-(4-chlorobenzyl) indole (III), which is treated with oxalyl chloride in a hot aprotic solvent yielding the intermediate acid chloride (IV). Finally, this compound is treated with pyridin-4-amine (V) in the same solvent.
| 【1】 Lebaut, G.; Menciu, C.; Kutscher, B.; Emig, P.; Szelenyi, S.; Brune, K. (Asta Medica AG); N-Substd. indol-3-glyoxylamide with antiasthmatic, antiallergic and immunosuppressive/immunomodulating effect. DE 19636150; EP 0931063; JP 2000505098; US 6008231; WO 9809946 . |
| 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) | 15292 | Indole; 1H-indole | 120-72-9 | C8H7N | 详情 | 详情 |
| (II) | 10356 | 1-Chloro-4-(chloromethyl)benzene; 4-Chlorobenzyl chloride | 104-83-6 | C7H6Cl2 | 详情 | 详情 |
| (III) | 30441 | 1-(4-chlorobenzyl)-1H-indole | C15H12ClN | 详情 | 详情 | |
| (IV) | 30442 | 2-[1-(4-chlorobenzyl)-1H-indol-3-yl]-2-oxoacetyl chloride | C17H11Cl2NO2 | 详情 | 详情 | |
| (V) | 25661 | 4-pyridinamine; 4-aminopyridine | 5044-74-5 | C5H6N2 | 详情 | 详情 |
Extended Information