Affiliation:
1. College of Chemistry and Chemical Engineering, Shaoxing University, Shaoxing 312000, People's Republic of China
2. Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, People's Republic of China
Abstract
AbstractThe development of highly efficient C–C bond formation methods for the synthesis of ethyl 2-(2,4-dichloro-5-fluorobenzoyl)-3-(dimethylamino)acrylate 1 in continuous flow processes has been described, which is based on the concept of rapid and efficient activation of carboxylic acid. 2,4-Dichloro-5-fluorobenzoic acid is rapidly converted into highly reactive 2,4-dichloro-5-fluorobenzoyl chloride by treating with inexpensive and less-toxic solid bis(trichloromethyl)carbonate. And then it rapidly reacts with ethyl 3-(dimethylamino)acrylate to afford the desired 1. This process can be performed under mild conditions. Compared with the traditional tank reactor process, less raw material consumption, higher product yield, less reaction time, higher operation safety ensured by more the environmentally friendly procedure, and process continuity are achieved in the continuous-flow system.
Funder
Public Projects of Zhejiang Province
National Natural Science Foundation of China
Subject
General Earth and Planetary Sciences,General Environmental Science
Reference20 articles.
1. Bacterial infections in cirrhosis: epidemiological changes with invasive procedures and norfloxacin prophylaxis;J Fernández;Hepatology,2002
2. Ciprofloxacin;A Tutkun;Arch Otolaryngol Head Neck Surg,1994
3. Pefloxacin in histoid leprosy;P M Mahajan;Int J Lepr Other Mycobact Dis,1994
4. Fleroxacin clinical pharmacokinetics;A E Stuck;Clin Pharmacokinet,1992
5. Synthesis of 2,4-dichloro-5-fluorobenzoyl chloriedas Intermediate of ciproflxacin;X M Wen;J Ji Ning Med College,2000