Synthetic approaches and pharmaceutical applications of chloro-containing molecules for drug discovery: A critical review

At present more than 250 FDA approved chlorine containing drugs were available in the market and many pharmaceutically important drug candidates in pre-clinical trials. Thus, it is quite obvious to expect that in coming decades there will be an even greater number of new chlorine-containing pharmaceuticals in market. Chlorinated compounds represent the family of compounds promising for use in medicinal chemistry. This review describes the recent advances in the synthesis of chlorine containing heterocyclic compounds as diverse biological agents and drugs in the pharmaceutical industries for the inspiration of the discovery and development of more potent and effective chlorinated drugs against numerous death-causing diseases. [Display omitted] •The applications of chlorine in medicinal chemistry is one of the fastest growing hot research areas in the chemistry community.•More than 250 FDA approved chloro-containing drugs are in the market.•This review summarizes nearly 130 FDA approved drugs against diverse biological agents.•Discussions of the SAR of potent drugs were included.