Barlaam, Bernard; De Savi, Chris; Dishington, Allan; Drew, Lisa; Ferguson, Andrew D.; Ferguson, Douglas; Gu, Chungang; Hande, Sudhir; Hassall, Lorraine; Hawkins, Janet; Hird, Alexander W.; Holmes, Jane; Lamb, Michelle L.; Lister, Andrew S.; McGuire, Thomas M.; Moore, Jane E.; O’Connell, Nichole; Patel, Anil; Pike, Kurt G.; Sarkar, Ujjal; Shao, Wenlin; Stead, Darren; Varnes, Jeffrey G.; Vasbinder, Melissa M.; Wang, Lei; Wu, Liangwei; Xue, Lin; Yang, Bin; Yao, Tieguang published their research in Journal of Medicinal Chemistry in 2021. The article was titled 《Discovery of a Series of 7-Azaindoles as Potent and Highly Selective CDK9 Inhibitors for Transient Target Engagement》.Application of 25637-16-5 The article contains the following contents:
Optimization of a series of azabenzimidazole54387894As identified from screening hit 2 and the information gained from a co-crystal structure of the azabenzimidazole-based lead 6 bound to CDK9 led to the discovery of azaindoles as highly potent and selective CDK9 inhibitors. With the goal of discovering a highly selective and potent CDK9 inhibitor administered i.v. that would enable transient target engagement of CDK9 for the treatment of hematol. malignancies, further optimization focusing on physicochem. and pharmacokinetic properties led to azaindoles 38 (I) and 39 (II). These compounds are highly potent and selective CDK9 inhibitors having short half-lives in rodents, suitable phys. properties for i.v. administration, and the potential to achieve profound but transient inhibition of CDK9 in vivo. The results came from multiple reactions, including the reaction of 4-Bromotetrahydropyran(cas: 25637-16-5Application of 25637-16-5)
4-Bromotetrahydropyran(cas: 25637-16-5) is often used as reactant for: nickel-catalyzed alkyl-alkyl Suzuki coupling reactions with boron reagents, preparation of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans; preparation of aliphatic hydrocarbons via nickel-catalyzed Suzuki cross-coupling with alkylboranes.Application of 25637-16-5
Referemce:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics