Modern advances in heterocyclic chemistry in drug discovery. Issue 28 (10th June 2016)

• Record Type: Journal Article
• Authors: Taylor, Alexandria P.; Robinson, Ralph P.; Fobian, Yvette M.; Blakemore, David C.; Jones, Lyn H.; Fadeyi, Olugbeminiyi
• Is Part Of: Organic & biomolecular chemistry. Volume 14:Issue 28(2016)
• Page Start: 6611
• Page End: 6637
• Publication Date: 2016-06-10
• Subjects: Chemistry, Organic -- Periodicals; Bioorganic chemistry -- Periodicals; Chemistry, Physical organic -- Periodicals; 547
• DOI: 10.1039/c6ob00936k
• Languages: English
• ISSNs: 1477-0520

Abstract

Abstract : New advances in functionalized heterocyclic chemistry are of critical importance to the medicinal chemist as it provides the ability to expand the available drug-like chemical space and drive more efficient delivery of drug discovery programs. Abstract : New advances in synthetic methodologies that allow rapid access to a wide variety of functionalized heterocyclic compounds are of critical importance to the medicinal chemist as it provides the ability to expand the available drug-like chemical space and drive more efficient delivery of drug discovery programs. Furthermore, the development of robust synthetic routes that can readily generate bulk quantities of a desired compound help to accelerate the drug development process. While established synthetic methodologies are commonly utilized during the course of a drug discovery program, the development of innovative heterocyclic syntheses that allow for different bond forming strategies are having a significant impact in the pharmaceutical industry. This review will focus on recent applications of new methodologies in C–H activation, photoredox chemistry, borrowing hydrogen catalysis, multicomponent reactions, regio- and stereoselective syntheses, as well as other new, innovative general syntheses for the formation and functionalization of heterocycles that have helped drive project delivery. Additionally, the importance and value of collaborations between industry and academia in shaping the development of innovative synthetic approaches to functionalized heterocycles that are of greatest interest to the pharmaceutical industry will be highlighted.