|
【结 构 式】 
|
【药物名称】 【化学名称】 【CA登记号】 【 分 子 式 】C24H20N2O7S 【 分 子 量 】480.5002 |
【开发单位】 【药理作用】0 |
合成路线1
Thiocolchicine (II) was prepared from colchicine (I) by treatment with sodium methylthiolate. Then, hydrolysis of acetamide group with methanolic HCl afforded deacetyl thiocolchicine (III). Subsequent acylation with p-nitrobenzoyl chloride (IV) in the presence of pyridine provided amide (V), which was demethylated with excess BBr3 to give the corresponding triphenol.
| 【1】 Guan, J.; et al.; Antitumor agents. 185. Synthesis and biological evaluation of tridemethylthiocolchicine analogues as novel topoisomerase II inhibitors. J Med Chem 1998, 41, 11, 1956. |
| 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) | 18479 | N-[(7S)-1,2,3,10-tetramethoxy-9-oxo-5,6,7,9-tetrahydrobenzo[a]heptalen-7-yl]acetamide | 64-86-8 | C22H25NO6 | 详情 | 详情 |
| (II) | 18480 | N-[(7S)-1,2,3-trimethoxy-10-(methylsulfanyl)-9-oxo-5,6,7,9-tetrahydrobenzo[a]heptalen-7-yl]acetamide | C22H25NO5S | 详情 | 详情 | |
| (III) | 18481 | (7S)-7-amino-1,2,3-trimethoxy-10-(methylsulfanyl)-6,7-dihydrobenzo[a]heptalen-9(5H)-one | C20H23NO4S | 详情 | 详情 | |
| (IV) | 18941 | p-nitrobenzoyl chloride; 4-nitrobenzoyl chloride | 122-04-3 | C7H4ClNO3 | 详情 | 详情 |
| (V) | 18483 | 4-nitro-N-[(7S)-1,2,3-trimethoxy-10-(methylsulfanyl)-9-oxo-5,6,7,9-tetrahydrobenzo[a]heptalen-7-yl]benzamide | C27H26N2O7S | 详情 | 详情 |
Extended Information