93106-60-6 (恩诺沙星,Enrofloxacin)

_97%

反应条件：

1.1 Catalysts: Molybdate(42-), triacontakis[μ-(acetato-κO:κO′)]doheptacontaaquaoctacontahecta-μ… Solvents: Water ; 30 min, reflux

参考文献：

Fast and green method to synthesis of quinolone carboxylic acid derivatives using giant-ball nanoporous isopolyoxomolybdate as highly efficient recyclable catalyst in refluxing water

Mirzaie, Yahya; Lari, Jalil; Vahedi, Hooshang; Hakimi, Mohammad; Nakhaei, Ahmad; et al, Journal of the Mexican Chemical Society, 2017, 61(1), 35-40

合成路线：1 步

_97%

反应条件：

1.1 Catalysts: Zirconium dioxide (sulfonic acid derivative absorbed on ferrite) Solvents: Water ; 19 min, reflux

参考文献：

Nano-Fe3O4@ZrO2-SO3H as Highly Efficient Recyclable Catalyst for the Green Synthesis of Fluoroquinolones

Nakhaei, Ahmad; Ramezani, Shirin; Shams-Najafi, Sayyed Jalal; Farsinejad, Sadaf, Letters in Organic Chemistry, 2018, 15(9), 739-746

合成路线：1 步

85721-33-1

75-03-6

_97%

反应条件：

1.1 Reagents: Triethylamine Solvents: Dimethylformamide ; rt → 80 °C; 2 h, 80 °C
1.2 Reagents: Water ; cooled

参考文献：

Synthesis of labeled enrofloxacin-D5

Xu, Zhong-jie; Lu, Wei-jing; Lu, Hao, Jingxi Huagong, 2012, 29(11), 1050-1052

合成路线：1 步

_93%

反应条件：

1.1 25 min, 150 °C

参考文献：

Conventional and microwave-assisted synthesis of quinolone carboxylic acid derivatives

Mirzaie, Y.; Lari, J.; Vahedi, H.; Hakimi, M., Russian Journal of General Chemistry, 2016, 86(12), 2865-2869

合成路线：1 步

_92%

反应条件：

1.1 Catalysts: Aluminum bromide Solvents: Ethanol ; 4 h, rt → 75 °C
1.2 Reagents: Sodium hydroxide Solvents: Water ; 30 min, 70 °C
1.3 Reagents: Hydrochloric acid Solvents: Water ; neutralized

参考文献：

Preparation of norfloxacin, ciprofloxacin and enrofloxacin

, China, , ,

合成路线：1 步

105112-41-2

_92%

反应条件：

1.1 Catalysts: Aluminum chloride Solvents: Isoamyl alcohol ; 8 h, 140 °C
1.2 Reagents: Hydrochloric acid Solvents: Water
1.3 Reagents: Hydroxide ; pH 7.2 - 7.3

参考文献：

Methods for preparation of norfloxacin, ciprofloxacin and enrofloxacin

, China, , ,

合成路线：1 步

105392-26-5

_89%

反应条件：

1.1 Reagents: Sodium hydroxide Solvents: Toluene ; 4 h, reflux
1.2 Reagents: Hydrochloric acid Solvents: Water
1.3 Solvents: Water ; 1 h, reflux; 14 h, 115 °C

参考文献：

Convenient one pot synthesis of some fluoroquinolones in aqueous media

Abaee, M. Saeed; Sharifi, Ruhollah; Borhani, Shahin; Heravi, Majid M.; Motahari, Hossein, Heterocyclic Communications, 2005, 11(5), 415-418

合成路线：1 步

_72%

反应条件：

1.1 Catalysts: Cerium trichloride heptahydrate Solvents: Water ; rt → 100 °C; 10 h, 99 °C
1.2 Reagents: Methanol ; 0.5 h, reflux; reflux → 5 °C; 1 h, 5 - 8 °C

参考文献：

Process for preparation of carbostyril medicines

, China, , ,

合成路线：1 步

93107-08-5

74-96-4

_70%

反应条件：

1.1 Reagents: Diisopropylethylamine Catalysts: Potassium iodide Solvents: Acetonitrile , Water ; 0 °C; 16 h, rt

参考文献：

Pharmacological characterization of 7-(4-(piperazin-1-yl)) ciprofloxacin derivatives: antibacterial activity, cellular accumulation, susceptibility to efflux transporters, and intracellular activity

Marquez, Beatrice; Pourcelle, Vincent; Vallet, Coralie M.; Mingeot-Leclercq, Marie-Paule; Tulkens, Paul M.; et al, Pharmaceutical Research, 2014, 31(5), 1290-1301

合成路线：1 步

98349-25-8

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Water ; 10 h, 90 - 95 °C; 90 °C → rt
1.2 Reagents: Hydrochloric acid Solvents: Water ; 3 h, pH 7.5, rt

参考文献：

Process for the preparation of fluoroquinolone-3-carboxylic acids via amination of alkyl fluoro(haloquinolone)carboxylates with amines

, France, , ,

合成路线：1 步

86483-53-6

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Dimethylformamide ; 2 h, 120 °C
1.2 Reagents: Acetic acid , Hydrochloric acid Solvents: Water ; 4 h, 90 °C
1.3 Solvents: Isoamyl alcohol ; 6 h, 110 - 115 °C

参考文献：

Synthesis of derivatives of 1-ethyl-6-fluoro-7-(1-piperazinyl)-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid

Xie, Jiangang; Liao, Xincheng; Qu, Lingbo; Tian, Mengchao, Zhengzhou Daxue Xuebao, 2003, 35(3), 75-78

合成路线：1 步

107884-20-8

反应条件：

1.1 Reagents: Sodium hydroxide Solvents: Water
1.2 Reagents: Acetic acid

参考文献：

An improved process for the preparation of quinolone derivatives, e.g. ciprofloxacin

, World Intellectual Property Organization, , ,

合成路线：1 步

参考文献：

New process for the preparation of 1-cyclopropyl-3-quinolinecarboxylic acid derivatives

, Spain, , ,

合成路线：1 步

反应条件：

1.1 Solvents: Dimethyl sulfoxide

参考文献：

Cycloaracylation of enamines. I. Synthesis of 4-quinolone-3-carboxylic acids

Grohe, Klaus; Heitzer, Helmut, Liebigs Annalen der Chemie, 1987, (1), 29-37

合成路线：1 步

参考文献：

Preparation of specific conjugation bridge linkers and immunoconjugates and methods of using them

, World Intellectual Property Organization, , ,

合成路线：1 步

参考文献：

Preparation of bridge linkers used for specific conjugation of two or more cytotoxic agents to a cell-binding molecule

, World Intellectual Property Organization, , ,

合成路线：1 步

参考文献：

Preparation of bridge linkers used for specific conjugation of a cytotoxic agent to a cell-binding molecule

, World Intellectual Property Organization, , ,

合成路线：1 步

参考文献：

Preparation of novel bridge linkers containing an acetylenedicarbonyl group for specific conjugation of a cytotoxic agent to a cell-binding molecule

, World Intellectual Property Organization, , ,

合成路线：1 步