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【结 构 式】 
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【药物名称】 【化学名称】N-Isopropyl-2-(1-methyl-2-phenyl-1H-indol-3-yl)-N-(pyridin-4-ylmethyl)acetamide 【CA登记号】 【 分 子 式 】C26H27N3O 【 分 子 量 】397.52459 |
【开发单位】Merck & Co. (Originator) 【药理作用】Oncolytic Drugs, Farnesyl Transferase Inhibitors, Inhibitors of Signal Transduction Pathways |
合成路线1
Reductive amination of pyridine-4-carbaldehyde (I) with isopropylamine (II) in the presence of NaBH4 furnished the secondary amine (III). This was then acylated with the indoleacetic acid (IV) using PyBOP as the coupling reagent to yield the target amide.
| 【1】 Lumma, W.C.; Quigley, A.G.; Sisko, J.T.; et al.; 2-Arylindole-3-acetamides as FPP-competitive inhibitors of farnesyltransferase. 221st ACS Natl Meet (April 1 2001, San Diego) 2001, Abst MEDI 154. |
| 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) | 17203 | 4-Pyridinecarboxaldehyde; isonicotinaldehyde | 872-85-5 | C6H5NO | 详情 | 详情 |
| (II) | 23933 | 2-Propanamine; Isopropylamine | 75-31-0 | C3H9N | 详情 | 详情 |
| (III) | 50896 | N-isopropyl-N-(4-pyridinylmethyl)amine; N-(4-pyridinylmethyl)-2-propanamine | C9H14N2 | 详情 | 详情 | |
| (IV) | 50897 | 2-(1-methyl-2-phenyl-1H-indol-3-yl)acetic acid | C17H15NO2 | 详情 | 详情 |
Extended Information