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CAS 1159908-18-5
(3S,4S)-4-(((R)-1-phenylethyl)amino)-1-tosylpyrrolidin-3-ol
登记编号：FINA-035
应用背景（按来源药适应症）
外耳炎非那沙星分泌性中耳炎非那沙星中耳炎非那沙星泌尿系统感染非那沙星肾盂肾炎非那沙星革兰氏阴性细菌感染非那沙星
来源药（使用该中间体的合成路线）
| 品种 | 梯队 | 到期年 |
|---|---|---|
| 非那沙星Finafloxacin | Tier C · 观察 / 贸易 | - |
合成路线中的位置（上下游链）
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2,4-dichloro-3-cyano-5-fluorobenzoyl chloride→(Z)-ethyl 3-(dimethylamino)acrylate→ethyl 2-(2,4-dichloro-3-cyano-5-fluorobenzoyl)-3-(dimethylamino)acrylate→cyclopropanamine→ethyl 3-(cyclopropylamino)-2-(2,4-dichloro-3-cyano-5-fluorobenzoyl)acrylate→ethyl 7-chloro-8-cyano-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylate→(E)-but-2-ene-1,4-diol→1-tosyl-2,5-dihydro-1H-pyrrole→3-tosyl-6-oxa-3-azabicyclo[3.1.0]hexane→2,4-dichloro-1-fluorobenzene→1-(2,4-dichloro-5-fluorophenyl)ethanone→2,4-dichloro-5-fluorobenzoic acid→2,4-dichloro-5-fluoro-3-nitrobenzoic acid→methyl 2,4-dichloro-5-fluoro-3-nitrobenzoate→methyl 3-amino-2,4-dichloro-5-fluorobenzoate→methyl 2,4-dichloro-3-cyano-5-fluorobenzoate→2,4-dichloro-3-cyano-5-fluorobenzoic acid→(4aS,7aS)-tert-butyl hexahydropyrrolo[3,4-b][1,4]oxazine-4(4aH)-carboxylate→(4aS,7aS)-tert-butyl 6-(8-cyano-1-cyclopropyl-3-(ethoxycarbonyl)-6-fluoro-4-oxo-1,4-dihydroquinolin-7-yl)hexahydropyrrolo[3,4-b][1,4]oxazine-4(4aH)-carboxylate→7-((4aS,7aS)-4-(tert-butoxycarbonyl)hexahydropyrrolo[3,4-b][1,4]oxazin-6(2H)-yl)-8-cyano-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid→(E)-1,4-dichlorobut-2-ene→(R)-1-phenylethan-1-amine→(3S,4S)-4-(((R)-1-phenylethyl)amino)-1-tosylpyrrolidin-3-ol→2-chloroacetyl chloride→2-chloro-N-((3S,4S)-4-hydroxy-1-tosylpyrrolidin-3-yl)-N-((R)-1-phenylethyl)acetamide→(4aS,7aS)-4-((R)-1-phenylethyl)-6-tosylhexahydropyrrolo[3,4-b][1,4]oxazin-3(2H)-one→(4aS,7aS)-4-((R)-1-phenylethyl)-6-tosyloctahydropyrrolo[3,4-b][1,4]oxazine→(4aS,7aS)-6-tosyloctahydropyrrolo[3,4-b][1,4]oxazine→(4aS,7aS)-tert-butyl 6-tosylhexahydropyrrolo[3,4-b][1,4]oxazine-4(4aH)-carboxylate
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