64622-16-8Relevant articles and documents
Discovery of N-(Indazol-3-yl)piperidine-4-carboxylic Acids as ROR?3t Allosteric Inhibitors for Autoimmune Diseases
Anthony, Neville,Azevedo, Rita,Barr, Kenneth,Cals, Jos,Correll, Craig C.,Daniels, Matthew,Deshmukh, Sujal,Ferguson, Heidi,Hegde, Laxminarayan G.,Karstens, Willem Jan,Lapointe, Blair T.,MacLean, John,Moy, Lily Y.,Nagpal, Sunil,Oubrie, Arthur,Palte, Rachel L.,Parthasarathy, Gopal,Richard Miller, J.,Sciammetta, Nunzio,Simov, Vladimir,Van Der Stelt, Mario,Van Eenenaam, Hans,Wesley Trotter, B.,Woodhouse, Janice D.,Zhang, Hongjun
supporting information, (2020/02/06)
The clinical success of anti-IL-17 monoclonal antibodies (i.e., Cosentyx and Taltz) has validated Th17 pathway modulation for the treatment of autoimmune diseases. The nuclear hormone receptor RORγt is a master regulator of Th17 cells and affects the prod
Palladium-catalyzed ortho-C(sp2)[sbnd]H bromination of benzaldehydes via a monodentate transient directing group strategy
Yong, Qiyun,Sun, Bing,Zhang, Fang-Lin
supporting information, (2019/11/03)
A facile and efficient monodentate transient directing group strategy was developed to enable the palladium-catalyzed ortho-C(sp2)[sbnd]H bromination of benzaldehydes. A broad scope of benzaldehydes were transformed into the desired products by employing 2-amino-5-chlorobenzotrifluoride as a monodentate transient directing group, demonstrating good functional group tolerance. Mild reaction conditions and no requirement for a silver salt are also features of this strategy.
Diverse ortho-C(sp2)-H functionalization of benzaldehydes using transient directing groups
Liu, Xi-Hai,Park, Hojoon,Hu, Jun-Hao,Hu, Yan,Zhang, Qun-Liang,Wang, Bao-Long,Sun, Bing,Yeung, Kap-Sun,Zhang, Fang-Lin,Yu, Jin-Quan
supporting information, p. 888 - 896 (2017/05/16)
Pd-catalyzed C-H functionalizations promoted by transient directing groups remain largely limited to C-H arylation only. Herein, we report a diverse set of ortho-C(sp2)-H functionalizations of benzaldehyde substrates using the transient directing group strategy. Without installing any auxiliary directing group, Pd(II)-catalyzed C-H arylation, chlorination, bromination, and Ir(III)-catalyzed amidation, could be achieved on benzaldehyde substrates. The transient directing groups formed in situ via imine linkage can override other coordinating functional groups capable of directing C-H activation or catalyst poisoning, significantly expanding the scope for metal-catalyzed C-H functionalization of benzaldehydes. The utility of this approach is demonstrated through multiple applications, including late-stage diversification of a drug analogue.