Kinetic Resolution of 1,
<scp>2‐Diamines</scp>
via Organocatalyzed Asymmetric Electrophilic Aminations of Anilines
作者:Jinglei Xie、Zheng Guo、Wei Liu、Dekun Zhang、Yu‐Peng He、Xiaoyu Yang
DOI:10.1002/cjoc.202200125
日期:2022.7.15
efficient kinetic resolution (KR) protocol for 1,2-diamines has been developed through asymmetric electrophilic aminations of anilines enabled by chiral phosphoric acid catalysis. A wide array of substituted 1,2-diamines were compatible with this method, generating both the recovered staring materials and the amination products with high enantioselectivities (with s-factor up to 218). Notably, this method
The present invention relates to compounds and derivatives thereof, their synthesis, and their use as glucocorticoid receptor modulators. The compounds of the instant invention are ligands for glucocorticoid receptors and as such may be useful for treatment or prevention of a variety of conditions related to glucocorticoid functioning including rheumatoid arthritis, osteoarthritis, allery, asthma, pneumonia, dermatitis, eczema, psoriasis, lupus, colitis, inflammatory bowel disease, multiple sclerosis, congenital neutropenia, Wegener's granulomatosis, Addison's Disease, Crohn's disease Cushing Syndrome, or as immunosuppressants in organ transplantation.
Imidazolines substituted at the 1- and either the 4-, or 5-position with phenyl and at the 2-position with alkyl or phenyl have been prepared in racemic form. They appear to be fairly stable compounds and potentially useful as scaffolds in medicinal chemistry.