Fluorine in medicinal chemistry: Recent therapeutic applications of fluorinated small molecules

Catalytic Nucleophilic Addition of 3, 5-Dialkyl-4-nitroisoxazoles to Trifluoromethyl Ketones on Water

“…[1,2] Particularly, some trifluoromethylsubstituted tertiary alcohols are important pharmaceuticals and agrochemicals, such as the critical anti-HIV drug (Efavirenz, I), [3] anticonvulsant II, [4] glucocorticoid agonist (BI-653048, III), [5] selective glucocorticoid receptor agonist (ZK-216348, IV), [6] anticancer agents V, [7] the platelet-activating factor antagonists VI [8] (Figure 1). Accordingly, the creation of bearing trifluoromethyl-substituted tertiary alcohols from readily available starting substrates under mild reaction conditions is of great synthetic and industrial interest.…”

“…2 Results and discussion 2,2, were chosen as the model substrates to optimize the reaction conditions at room temperature. The results are summarized in Table 1.…”

Synthesis and Antimicrobial Activities of New 1,2,4- Triazoles, Mannich Bases, Conazoles, and Fluoroquinolones

“…Thus, a single compound possessing more than one active group, each with varied form of activity, might be advantageous for the cure of bacterial diseases [6,7]. Heterocycle-and fluorine-containing compounds play a crucial role both in the research field of organic chemistry and in a variety of practical chemistry fields, such as, material science, medicinal chemistry, and pesticide chemistry [8][9][10][11][12]. 1,2,4-triazole is a five-membered heterocycle, and has a broad spectrum of biological properties containing anticancer [13,14], insecticidal [15], antifungal [16], anti-inflammatory [17], and plant growth regulating activities [18].…”

Regiospecific synthesis of new fatty N-acyl trihalomethylated pyrazoline derivatives from fatty acid methyl esters (FAMEs)

“…[1][2][3][4][5][6][7][8] Since the introduction of halogens and halogenated groups into organic molecules often confers significant and useful changes in their chemical, physical and biological properties, 9 the development of new methods for synthesizing halogenated compounds recently has attracted considerable interest. Among the most convenient of these methods is the use of starting materials containing halogens, including halogenated 1,3-dieletrophiles in the form of trihalomethylated β-diketones and trihalomethylated α-β-unsaturated ketones (as 4-alkoxy-1,1,1-trihalo-3-alken-2-ones), which are regiospecific synthons for 5-trihalomethyl-1H-pyrazoles and for a variety of halomethyl-substituted heterocyclic compounds.…”