|
【结 构 式】 
|
【药物名称】R-123942 【化学名称】N-[1-[6-(1,2,4-Thiadiazol-5-yl)pyridazin-3-yl]piperidin-4-yl]-N-[3-(trifluoromethyl)phenyl]amine 【CA登记号】193957-04-9 【 分 子 式 】C18H17F3N6S 【 分 子 量 】406.43559 |
【开发单位】Janssen (Originator) 【药理作用】Lung Cancer Therapy, Oncolytic Drugs, Angiogenesis Inhibitors |
合成路线1
Treatment of 3-chloro-6-methylpyridazine (I) with thionyl chloride followed by reaction with imino derivative (II) in CH2Cl2 provides thiadiazolyl pyridazine derivative (III), which is then condensed with amine (IV) in the presence of Na2CO3 in DMF.
| 【1】 Stokbroekx, R.A.; Van der Aa, M.J.M.; Willems, M.; Meerpoel, L.; Luyckx, M.G.M.; Tuman, R.W. (Janssen Pharmaceutica NV); Angiogenesis inhibiting pyridazinamines. EP 0876366; JP 2000503014; US 5985878; WO 9726258 . |
| 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) | 13495 | 3-Chloro-6-methylpyridazine | 1121-79-5 | C5H5ClN2 | 详情 | 详情 |
| (II) | 15369 | Iminoformamide; Methanimidamide | 463-52-5 | CH4N2 | 详情 | 详情 |
| (III) | 47583 | 3-chloro-6-(1,2,4-thiadiazol-5-yl)pyridazine | C6H3ClN4S | 详情 | 详情 | |
| (IV) | 47584 | N-(4-piperidinyl)-N-[3-(trifluoromethyl)phenyl]amine; N-[3-(trifluoromethyl)phenyl]-4-piperidinamine | C12H15F3N2 | 详情 | 详情 |
Extended Information