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【结 构 式】 
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【分子编号】53071 【品名】7-[(3R)-3-(aminomethyl)-3-methyl-4-oxopyrrolidinyl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro[1,8]naphthyridine-3-carboxylic acid 【CA登记号】n/a |
【 分 子 式 】C18H19FN4O4 【 分 子 量 】374.3718232 【元素组成】C 57.75% H 5.12% F 5.07% N 14.97% O 17.09% |
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：(XXI)Condensation of the intermediate pyrrolidine (XII) with the fluoronaphthyridine (XIX) provided adduct (XX). Simultaneous cleavage of the ketal and N-Boc groups under acidic conditions gave (XXI). The keto group of (XXI) was finally converted to the title O-methyloxime by treatment with O-methylhydroxylamine in pyridine.
| 【1】 Lee, C.-W.; et al.; Synthesis antibacterial activities of DW286, a new fluoronaphthyridone antibiotic as an enantiomer. 41st Intersci Conf Antimicrob Agents Chemother (Dec 16 2001, Chicago) 2001, Abst F-553. |
| 【2】 Yoon, S.J.; Chung, Y.H.; Lee, C.W.; Choi, D.R.; Lee, J.S.; Yang, W.Y.; Kim, N.D.; Jin, Y.H.; Song, W.J.; Kim, I.H.; Shin, J.H. (Dong-Wha Pharmaceuticals Industry Co. Ltd); Optically active quinoline carboxylic acid derivs. having 7-pyrrolidine substitutes causing optical activity and a process for preparing thereof. WO 0071541 . |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (XII) | 53063 | tert-butyl [(4S)-4,8,8-trimethyl-6,10-dioxa-2-azaspiro[4.5]dec-4-yl]methylcarbamate | n/a | C16H30N2O4 | 详情 | 详情 |
| (XIX) | 17034 | 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro[1,8]naphthyridine-3-carboxylic acid | 100361-18-0 | C12H8ClFN2O3 | 详情 | 详情 |
| (XX) | 53070 | 7-((4R)-4-{[(tert-butoxycarbonyl)amino]methyl}-4,8,8-trimethyl-6,10-dioxa-2-azaspiro[4.5]dec-2-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro[1,8]naphthyridine-3-carboxylic acid | n/a | C28H37FN4O7 | 详情 | 详情 |
| (XXI) | 53071 | 7-[(3R)-3-(aminomethyl)-3-methyl-4-oxopyrrolidinyl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro[1,8]naphthyridine-3-carboxylic acid | n/a | C18H19FN4O4 | 详情 | 详情 |
Extended Information