36603-28-8Relevant articles and documents
Ligand-Controlled Regiodivergent Catalytic Amidation of Unactivated Secondary Alkyl Bromides
Tortajada, Andreu,Menezes Correia, Jose Tiago,Serrano, Eloisa,Monleón, Alicia,Tampieri, Alberto,Day, Craig S.,Juliá-Hernández, Francisco,Martin, Ruben
, p. 10223 - 10227 (2021/08/24)
A regiodivergent Ni-catalyzed amidation of unactivated secondary alkyl bromides is described. The site-selectivity of the amidation event is dictated by subtle differences on the ligand backbone, allowing introduction of the amide function at either the original sp3 carbon-halide bond or at distal sp3 C-H sites within an alkyl side-chain via chain-walking scenarios.
Nickel-Catalyzed Reductive Amidation of Unactivated Alkyl Bromides
Serrano, Eloisa,Martin, Ruben
supporting information, p. 11207 - 11211 (2016/10/13)
A user-friendly, nickel-catalyzed reductive amidation of unactivated primary, secondary, and tertiary alkyl bromides with isocyanates is described. This catalytic strategy offers an efficient synthesis of a wide range of aliphatic amides under mild conditions and with an excellent chemoselectivity profile while avoiding the use of stoichiometric and sensitive organometallic reagents.
Discovery and biological evaluation of novel cyanoguanidine P2X7 antagonists with analgesic activity in a rat model of neuropathic pain
Perez-Medrano, Arturo,Donnelly-Roberts, Diana L.,Honore, Prisca,Hsieh, Gin C.,Namovic, Marian T.,Peddi, Sridhar,Shuai, Qi,Wang, Ying,Faltynek, Connie R.,Jarvis, Michael F.,Carroll, William A.
scheme or table, p. 3366 - 3376 (2010/04/03)
We disclose the design of a novel series of cyanoguanidines that are potent (IC50 ? 10-100 nM) and selective (≥100-fold) P2X7 receptor antagonists against the other P2 receptor subtypes such as the P2Y2, P2X4, and P2X3. We also found that these P2X7 antagonists effectively reduced nociception in a rat model of neuropathic pain (Chung model). Particularly, analogue 53 proved to be effective in the Chung model, with an ED50 of 38 μmol/kg after intraperitoneal administration. In addition compound 53 exhibited antiallodynic effects following oral administration and maintained its efficacy following repeated administration in the Chung model. These results suggest an important role of P2X7 receptors in neuropathic pain and therefore a potential use of P2X7 antagonists as novel therapeutic tools for the treatment of this type of pain.