《Expanding the Medicinal Chemist Toolbox: Comparing Seven C(sp2)-C(sp3) Cross-Coupling Methods by Library Synthesis》 was published in ACS Medicinal Chemistry Letters in 2020. These research results belong to Dombrowski, Amanda W.; Gesmundo, Nathan J.; Aguirre, Ana L.; Sarris, Katerina A.; Young, Jonathon M.; Bogdan, Andrew R.; Martin, M. Cynthia; Gedeon, Shasline; Wang, Ying. HPLC of Formula: 25637-16-5 The article mentions the following:
Despite recent advances in the field of C(sp2)-C(sp3) cross-couplings and the accompanying increase in publications, it can be hard to determine which method is appropriate for a given reaction when using the highly functionalized intermediates prevalent in medicinal chem. Thus a study was done comparing the ability of seven methods to directly install a diverse set of alkyl groups on “”drug-like”” aryl structures via parallel library synthesis. Each method showed substrates that it excelled at coupling compared with the other methods. When analyzing the reactions run across all of the methods, a reaction success rate of 50% was achieved. Whereas this is promising, there are still gaps in the scope of direct C(sp2)-C(sp3) coupling methods, like tertiary group installation. The results reported herein should be used to inform future syntheses, assess reaction scope, and encourage medicinal chemists to expand their synthetic toolbox. The results came from multiple reactions, including the reaction of 4-Bromotetrahydropyran(cas: 25637-16-5HPLC of Formula: 25637-16-5)
4-Bromotetrahydropyran(cas: 25637-16-5) is often used as reactant for: preparation of anthranilic acids as antibacterial agents with human serum albumin binding affinity; preparation of antiatherogenic antioxidant di-tert-butyldihydrobenzofuranols via Grignard reactions with di-tert-butyl(hydroxy)benzaldehyde derivatives; synthesis of gephyrotoxin via the Schmidt reaction.HPLC of Formula: 25637-16-5
Referemce:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics