DMSO-Catalyzed Late-Stage Chlorination of (Hetero)arenes
Ning Jiao describes the late-stage chlorination of various arenes through DMSO catalysis.
Chlorinated (hetero)arenes are widely used in organic synthesis and in pharmaceuticals. Professor Ning Jiao – an organic synthesis expert at Peking University (P. R. of China) – pointed out that Pfizer systematically screened more than 220,000 aryl derivatives and found that aromatic chlorination may change the physicochemical properties of drugs, such as pKa, dipole moment, as well as metabolic rate, therefore improving pharmacokinetic and pharmacological properties. Although some elegant chlorination reactions have been developed, these protocols suffer from either the high cost of the chlorinating reagents or harsh conditions. Professor Jiao mentioned that, therefore, the efficient and practical late-stage chlorination of bioactive molecules remains formidably challenging.
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