ethyl 7-(3-amino-1-pyrrolidinyl)-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro[1,8]naphthyridine-3-carboxylate -Drug Synthesis Database

【结构式】

【分子编号】20939

【品名】ethyl 7-(3-amino-1-pyrrolidinyl)-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro[1,8]naphthyridine-3-carboxylate

【CA登记号】

【分子式】C₂₁H₁₉F₃N₄O₃

【分子量】432.4022296

【元素组成】C 58.33% H 4.43% F 13.18% N 12.96% O 11.1%

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：(III)

Ethyl 7-chloro-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylate (I) is reacted with 3-aminopyrrolidine dihydrochloride (II), and then the resulting mixture is reacted with potassium hydroxide and p-toluenesulfonic acid monohydrate in order to obtain (rac)-7-(3-amino-1-pyrrolidinyl)-6-fluoro-1-(2,4-difluorophenyl)- 1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid p-toluenesulfonate hydrate.

参考文献中间体

合成目标

【1】 Soejima, R.; Shimada, K.; TOSUFLOXACIN TOSYLATE < Prop INNM >. Drugs Fut 1989, 14, 6, 536.
【2】 Kokei, T.; et al.; Chemical structure and physicochemical properties of (rac)-7-(3-amino-1-pyrrolidinyl)-6-fluoro-1-(2,4-difluorophenyl)-1,4- dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid p-toluensulfonate hydrate (T-3262). Iyakuhin Kenkyu 1988, 19, 682.
【3】 Narita, H.; et al.; Pyridonecarboxylic acids as antibacterial agents IV. Yakugaku Zasshi 1986, 106, 795.

中间体序号	中间体编号	品名	分子式	供应商	用于合成
(I)	15230	ethyl 7-chloro-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro[1,8]naphthyridine-3-carboxylate	C₁₇H₁₀ClF₃N₂O₃	详情	详情
(II)	20938	3-pyrrolidinamine; 3-pyrrolidinylamine	C₄H₁₀N₂	详情	详情
(III)	20939	ethyl 7-(3-amino-1-pyrrolidinyl)-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro[1,8]naphthyridine-3-carboxylate	C₂₁H₁₉F₃N₄O₃	详情	详情

Extended Information