|
【结 构 式】 
|
【药物名称】PD-166866 【化学名称】N-[2-Amino-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]-N'-(tert-butyl)urea 【CA登记号】192705-79-6 【 分 子 式 】C20H24N6O3 【 分 子 量 】396.45268 |
【开发单位】Pfizer (Originator) 【药理作用】Angiogenesis Inhibitors, Inhibitors of Signal Transduction Pathways, Tyrosine Kinase Inhibitors |
合成路线1
Condensation of pyrimidine carboxaldehyde (I) with 3,5-dimethoxy-phenylacetonitrile (II) using NaH in 2-ethoxyethanol provided the pyridopyrimidine (III). Then, regioselective condensation of (III) with tert-butyl isocyanate at the 7-amino group in the presence of NaH in DMF furnished the corresponding urea.
| 【1】 Connolly, C.J.C.; Schroeder, M.C.; Hamby, J.M.; et al.; Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors. J Med Chem 1997, 40, 15, 2296. |
| 【2】 Hamby, J.M.; Connolly, C.J.C.; Schroeder, M.C.; et al.; Discovery and structure-activity studies of a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors. Bioorg Med Chem Lett 1997, 7, 18, 2415. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| 16976 | tert-butylisocyanate; tert-butyl isocyanate; 2-isocyanato-2-methylpropane | 1609-86-5 | C5H9NO | 详情 | 详情 | |
| (I) | 26525 | 2,4-diamino-5-pyrimidinecarbaldehyde | C5H6N4O | 详情 | 详情 | |
| (II) | 26526 | 2-(3,5-dimethoxyphenyl)acetonitrile | 13388-75-5 | C10H11NO2 | 详情 | 详情 |
| (III) | 26527 | 2-amino-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-ylamine | C15H15N5O2 | 详情 | 详情 |
Extended Information