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【结 构 式】 
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【分子编号】43711 【品名】(4R)-3-formyl-2-(3-pyridinyl)-1,3-thiazolidine-4-carboxylic acid 【CA登记号】 |
【 分 子 式 】C10H10N2O3S 【 分 子 量 】238.26708 【元素组成】C 50.41% H 4.23% N 11.76% O 20.14% S 13.46% |
与该中间体有关的原料药合成路线共 1 条
合成路线1
该中间体在本合成路线中的序号：(IV)The cyclization of pyridine-3-carbaldehyde (II) with L-cysteine (I) in ethanol gives the thiazolidine derivative (III), which is treated with formic acid yielding the 3-formylthiazolidine derivative (IV). The cyclization of (IV) with 2-chloropropenenitrile (V) by means of acetic anhydride affords 3-(3-pyridil)-1H,3H-pyrrolo[1,2-c]thiazole-7-carbonitrile (VI), which is finally hydrolyzed to the target carboxamide by means of KOH in tert-butanol.
| 【1】 Fabre, J.-L.; Farge, D.; James, C.; Lavé, D. (Aventis SA); Novel 1H,3H-pyrrolo[1,2-c]thiazole derivs., their preparation and medicaments containing them. EP 0115979; US 4529728 . |
| 【2】 Lavé, D.; James, C.; Rajoharison, H.; Bost, P.E.; Cavero, I.; PYRROLO[1,2-c]THIAZOLE DERIVATIVES: POTENT PAF RECEPTOR ANTAGONISTS. Drugs Fut 1989, 14, 9, 891. |
| 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) | 14643 | L-cysteine; (R)-2-Amino-3-mercaptopropionic acid | 52-90-4 | C3H7NO2S | 详情 | 详情 |
| (II) | 12849 | Nicotinaldehyde; 3-Pyridinecarboxaldehyde | 500-22-1 | C6H5NO | 详情 | 详情 |
| (III) | 38634 | (4R)-2-(3-pyridinyl)-1,3-thiazolidine-4-carboxylic acid | C9H10N2O2S | 详情 | 详情 | |
| (IV) | 43711 | (4R)-3-formyl-2-(3-pyridinyl)-1,3-thiazolidine-4-carboxylic acid | C10H10N2O3S | 详情 | 详情 | |
| (V) | 12372 | 2-Chloroacrylonitrile | 920-37-6 | C3H2ClN | 详情 | 详情 |
| (VI) | 43712 | 3-(3-pyridinyl)-1H-pyrrolo[1,2-c][1,3]thiazole-7-carbonitrile | C12H9N3S | 详情 | 详情 |
Extended Information