|
【结 构 式】 
|
【药物名称】 【化学名称】N-(4-Methoxyphenylsulfanylcarbonyl)-L-glutamic acid 【CA登记号】192203-60-4, 192203-55-7 (undefined isomer) 【 分 子 式 】C13H15NO6S 【 分 子 量 】313.3316 |
【开发单位】Protherics (Originator) 【药理作用】Chemoprotective Agents, ONCOLYTIC DRUGS, Glutamate Carboxypeptidase Inhibitors |
合成路线1
The reaction of L-glutamic acid di tert-butyl ester (I) with 4-nitrophenyl chloroformate (II) by means of triethylamine in dichloromethane gives the corresponding carbamate (III), which is treated with 4-methoxythiophenol (IV) in dichloromethane to afford the thiocarbamate (V). Finally, this compound is treated with HCl.
| 【1】 Browne, P.J.; Burke, P.J.; Eno-Amooquaye, E.A.; Khan, T.H.; Osborn, H.M.I.; Searle, F.; Novel inhibitors of carboxypeptidase G2 (CPG2): Potential use in antibody-directed enzyme prodrug therapy. J Med Chem 1999, 42, 6, 951. |
| 【2】 Khan, T. (Aepact Ltd.); Drug therapy. WO 9720580 . |
| 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) | 29471 | di(tert-butyl) (2S)-2-aminopentanedioate | C13H25NO4 | 详情 | 详情 | |
| (II) | 16605 | 4-Nitrophenyl chloroformate; 1-[(Chlorocarbonyl)oxy]-4-nitrobenzene | 7693-46-1 | C7H4ClNO4 | 详情 | 详情 |
| (III) | 29472 | di(tert-butyl) (2S)-2-[[(4-nitrophenoxy)carbonyl]amino]pentanedioate | C20H28N2O8 | 详情 | 详情 | |
| (IV) | 25639 | 4-methoxyphenylhydrosulfide; 4-methoxybenzenethiol | 34320-82-6 | C7H8OS | 详情 | 详情 |
| (V) | 29473 | di(tert-butyl) (2S)-2-([[(4-methoxyphenyl)sulfanyl]carbonyl]amino)pentanedioate | C21H31NO6S | 详情 | 详情 |
Extended Information