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【结 构 式】 
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【分子编号】35518 【品名】benzhydryl (6R,7R)-7-amino-3-[(E)-3-chloro-1-propenyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate 【CA登记号】 |
【 分 子 式 】C23H21ClN2O3S 【 分 子 量 】440.95012 【元素组成】C 62.65% H 4.8% Cl 8.04% N 6.35% O 10.89% S 7.27% |
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：(XIX)The condensation of (XVIII) with 7-beta-amino-3-(3-chloro-1(E)-propenyl)-3-cephem-4-carboxylic acid diphenylmethyl ester (XIX) affords the expected amide (XX). The halogen exchange in (XX) with I2 and NaI in acetone gives the 3-iodo-1(E)-propenyl derivative (XXI), which is treated with quinoline (XXII) in dichloromethane to provide the quinolinium salt (XXIII). Finally, this compound is fully deprotected by a treatment with TFA and anisole.
| 【1】 Aszodi, J.; Dini, C.; Fauveau, P. (Aventis Pharma SA); Cephalosporins having in position 7 as substd. axymino radical, intermediates, processes for their preparation and their use as medicaments. CA 2111164; EP 0628562; JP 1994345776 . |
| 【2】 Dini, C.; Aszodi, J.; Synthesis of a dihydroxythiophene analogue of catechosporines. Bioorg Med Chem Lett 2000, 10, 4, 349. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (XVIII) | 35517 | 2-[(2-(benzhydryloxy)-1-[5-cyano-3,4-bis[(2-methoxyethoxy)methoxy]-2-thienyl]-2-oxoethoxy)imino]-2-[2-(tritylamino)-1,3-thiazol-4-yl]acetic acid | C52H48N4O11S2 | 详情 | 详情 | |
| (XIX) | 35518 | benzhydryl (6R,7R)-7-amino-3-[(E)-3-chloro-1-propenyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate | C23H21ClN2O3S | 详情 | 详情 | |
| (XX) | 35519 | C75H67ClN6O13S3 | 详情 | 详情 | ||
| (XXI) | 35520 | C75H67IN6O13S3 | 详情 | 详情 | ||
| (XXII) | 35521 | quinoline | 91-22-5 | C9H7N | 详情 | 详情 |
| (XXIII) | 35522 | C84H74N7O13S3 | 详情 | 详情 |
Extended Information