Abstract
While alkyl halides are valuable intermediates in synthetic organic chemistry, their use as bioactive motifs in drug discovery and medicinal chemistry is rare in comparison. This is likely attributable to the common misconception that these compounds are merely non-specific alkylators in biological systems. A number of chlorinated compounds in the pharmaceutical and food industries, as well as a growing number of halogenated marine natural products showing unique bioactivity, illustrate the role that chiral alkyl halides can play in drug discovery. Through a series of case studies, we demonstrate in this review that these motifs can indeed be stable under physiological conditions, and that halogenation can enhance bioactivity through both steric and electronic effects. Our hope is that, by placing such compounds in the minds of the chemical community, they may gain more traction in drug discovery and inspire more synthetic chemists to develop methods for selective halogenation.
Highlights
Alkyl halides are among the most versatile compounds in the chemical industry
This review has aimed to illustrate the medical benefit of chiral alkyl halides, as well as the
Especially chlorides, This review has aimed to illustrate the medical benefit of chiral alkyl halides, as well as the are often stable, which is underscored by the number of compounds in the clinic and food industry features of these play a key in their activity
Summary
Alkyl halides are among the most versatile compounds in the chemical industry. Small haloalkanes are some of the most commonly used solvents in chemical laboratories; chlorofluorocarbons have seen widespread use as refrigerants and propellants; and compounds containing both Br and F are often used in fire retardants. Halogenation of sppermeability, carbons is commonly used tofor increase lipophilicity, which can lead enhance the blood–brain barrier which is crucial drugs targeting the central nervous candidate [7]. Halogenation candrug enhance the blood–brain barrier permeability, which is crucial for drugs targeting the central nervous candidates [10]. Enhance the blood–brain barrier permeability, which is crucial for drugs targeting the central nervous system [9] These properties are mostused often exploited by the introduction of aryl chlorides into drug. Due to its small review aims to detail some compounds of medicinal significance that contain a halogen-bearing bearing stereogenic center. Due to its small these have reviewed previously [11], we will focus on alkyl chlorides and enhance the biological and pharmacological properties of drugs.
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