Development status of fluorinated pharmaceuticals and intermediates

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The application of fluorinated compounds in the field of medicine is becoming increasingly widespread. Fluorinated drugs have the characteristics of high efficiency, low toxicity, and easy metabolism. Although they are expensive, they are compensated for due to their small dosage and excellent performance. In the development of anti infective drugs, quinolone antibiotics such as norfloxacin and ciprofloxacin are commonly used in China.
Driven by the development of fluorinated pharmaceuticals, China has a large production of fluorinated pharmaceutical intermediates and a higher proportion of exports. At present, there are hundreds of fluorinated drugs both domestically and internationally, many of which have become very important varieties in synthetic drugs, such as fluoroquinolone antibiotics, antidepressant drug fluoxetine, antifungal drug fluconazole, etc. With the expiration of several patents of fluorine-containing blockbuster drugs, the market demand for related fluorine-containing intermediates will increase, especially in the fields of diabetes treatment, anti infection, anti-virus, surgical anesthetics, etc.
Fluorinated pharmaceutical intermediates mainly include aromatic fluorides and aliphatic fluorides, with aromatic fluorides being the main component. These fluorine-containing intermediates can also be used to prepare fluorine-containing pesticides, fluorine-containing dyes, etc. There are over 100 varieties with industrial scale production. At present, fluorinated aromatic pharmaceutical intermediates with good market prospects include 2,4-dichlorofluorobenzene, which is used for synthesizing anti infective quinolone drugs such as ciprofloxacin, floxacin, and norfloxacin; Fluorophenol used for synthesizing anti-inflammatory and anti rheumatic drugs such as thioninic acid and aldose reductase preparations such as Sorbinil; Fluorobenzoyl chloride used for the synthesis of cardiovascular and cerebrovascular drugs, including fluvastatin sodium; 4-bromo-2-fluoroaniline for the synthesis of anti-inflammatory drug ibuprofen; 4-chloro-4-fluorobenzophenone for the synthesis of medical deworming agent flubenzimidazole; In addition, aliphatic fluoride fluorobromomethane is an important intermediate of cephalosporin drugs such as cefuroxime. The above-mentioned fluoropharmaceutical intermediates still have strong competitiveness in the international market. In order to reduce costs, the international intermediate market has been shifted to Asia. The domestic and international market prospects for 2,4-dichlorofluorobenzene, 3-chloro-4-fluoroaniline, and trifluoromethylbenzene are quite optimistic, and the production scale is also relatively large. As a raw material for ciprofloxacin, 2,4-dichlorofluorobenzene has a domestic demand of 2000-3000 tons, which needs to be imported from the United States, Japan, Germany, and Italy; The important intermediate of quinolone drugs, 3-chloro-4-fluoroaniline, also has a significant gap.
At present, the market demand for aliphatic fluorine-containing pharmaceutical intermediates has soared. For example, ethyl trifluoroacetate is widely used to manufacture various pharmaceutical intermediates, including the drug "sitagliptin" for the treatment of diabetes, the specific drug "efeweren" for the treatment of AIDS, the specific drug "lisinopril" for cardiovascular and cerebrovascular diseases, the effective drug "finasteride" for the treatment of alopecia, and the antipyretic and analgesic drug "celecoxib", And the raw material of the main component of COVID-19 drug Paxlovid, Nematovir. As of the beginning of 2022, the domestic production capacity of ethyl trifluoroacetate is approximately 10000 tons. It is expected that by the end of 2023, after the release of new project production capacity, the domestic production capacity of ethyl trifluoroacetate will reach 30000 tons.

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