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【结 构 式】 
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【药物名称】RS-04, RS-481, RS-0481 【化学名称】(4R)-3-Benzoyl-N-[(1R)-1-phenylethyl]-4-thiazolidinecarboxamide 【CA登记号】104682-67-9 (undefined stereoch.) 【 分 子 式 】C19H20N2O2S 【 分 子 量 】340.44745 |
【开发单位】Sankyo (Originator) 【药理作用】IMMUNOMODULATING AGENTS, Immunostimulants, Oncolytic Drugs |
合成路线1
The benzoylation of thiazolidine-4(R)-carboxylic acid (I) with benzoyl chloride (II) by means of NaOH in acetone water gives the corresponding N-benzoyl derivative (III), which is then condensed with alpha-(R)-methylbenzylamine (IV) by means of isobutyl chloroformate and triethylamine in dichloromethane.
| 【1】 Matsui, T.; Nagano, M.; KLitamura, K.; Shimizu, F. (Sankyo Co., Ltd.); Amino acid derivatives having anti-tumor activity and compositions containing them.. EP 0173441; ES 8703830; US 4904680 . |
| 【2】 Castaner, J.; Prous, J.; RS-0481. Drugs Fut 1988, 13, 7, 627. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| 13423 | 1-[(Chlorocarbonyl)oxy]-2-methylpropane; Isobutyl chloroformate;isobutyl carbonochloridate | 543-27-1 | C5H9ClO2 | 详情 | 详情 | |
| (I) | 12899 | L-(-)-Thiazolidine-4-carboxylic acid; (4R)-1,3-Thiazolidine-4-carboxylic acid; (R)-(-)-Thiazolidine-4-carboxylic acid | 34592-47-7 | C4H7NO2S | 详情 | 详情 |
| (II) | 10463 | Benzoyl chloride | 98-88-4 | C7H5ClO | 详情 | 详情 |
| (III) | 22557 | (4R)-3-benzoyl-1,3-thiazolidine-4-carboxylic acid | C11H11NO3S | 详情 | 详情 | |
| (IV) | 10039 | (1R)-1-Phenylethylamine; (1R)-1-Phenyl-1-ethanamine.; L-alpha-Phenylethylamine | 3886-69-9 | C8H11N | 详情 | 详情 |
Extended Information