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Aryl fluorinated building blocks refer to a series of aromatic compounds possessing one or several fluorine atoms directly attached to the aromatic ring skeleton. Fluorine can provide many beneficial properties when incorporated into an Aryl. Firstly, fluorinated arenes are more lipophilic than their non-fluorinated counterparts, which can be used to advantage in drug development. Furthermore, fluorine is sometimes used as an isostere for hydrogen in medicinal chemistry. In addition, fluorinated compounds can be strategically used as transition state inhibitors.

Fluorinated molecules occupy a significant place in pharmaceutical, agrochemical, and material sciences, due to the unique properties of the fluorine atom. The introduction of a fluorine atom can modulate the properties of a bioactive molecule, which may lead to changes in solubility, lipophilicity, metabolic stability, conformation, hydrogen-bonding ability and chemical reactivity. Within the various fluorinated compounds, fluorinated alkenyl is of particular interest. It is not surprising to find a number of bioactive compounds with various pharmacological activities (such as anticancer, antimicrobial, anti-HIV, anti-diabetic) bearing this motif (Fig 1).

Alkyl fluorinated building blocks are a series of alkyl compounds substituted by fluorine atoms, which occur in a wide range of products. According to the number of fluorine substituents, they can be divided into monofluoro, polyfluoro and perfluorinated alkyl compounds. Current interest in fluorination chemistry is largely a consequence of the properties that fluorine substitution can impart on molecules, such as pharmaceuticals, agrochemicals, materials, and radiotracers for positron emission tomography. As many as 30-40% of agrochemicals and 20-25% of pharmaceuticals on the market are estimated to contain fluorine.

Azaindoles and their derivatives exhibit significant biological activities, hence they are widely concerned in terms of drug optimization strategies. The four azaindole positional isomers, which associate a pyridine and a pyrrole ring by a fused C-C bond, possess all of the criteria necessary to be excellent bioisosteres of the indole or purine systems. The physicochemical and pharmacological properties such as solubility, pKa and lipophilicity, target binding ability and toxicity can be modulated and finely tuned using the azaindole instead of other bicyclic fused heterocycles.

Introducing fluorine atom(s) into bioactive organic compounds has become a leading strategy for drug design and lead optimization. In drug synthesis strategy, fluorine is frequently employed to modify biologically relevant properties such as metabolic stability, basicity, lipophilicity and bioavailability. Additionally, the binding affinity of compounds to biological targets may also improve upon fluorination, therefore fluorine is considered an excellent candidate to serve as a bioisostere of hydroxyl, thiol or amine groups.