Aryl–secondary alkyl cross-coupling with aryl sulfonate esters as coupling partners remains a significant challenge. Efficient cross-coupling between aryl/alkenyl triflates and acyclicsecondary alkylboronic acids is realized for the first time to provide a series of sterically congested acyclicsecondary alkyl arenes/olefins in good to excellent yields. The employment of sterically bulky P,PO ligand L1/L2 is
The invention provides compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections. The compounds and compositions are useful for treating Pneumovirinae virus infection including Human respiratory syncytial virus infections.
SMALL MOLECULE CMKLR1 ANTAGONISTS IN INFLAMMATORY DISEASE
申请人:The Board of Trustees of the Leland Stanford Junior University
公开号:US20200345661A1
公开(公告)日:2020-11-05
α-NETA analogs are provided for the treatment of inflammatory disease.
α-NETA类似物用于治疗炎症性疾病。
KRAS G12C INHIBITORS AND METHODS OF USING THE SAME
申请人:AMGEN INC.
公开号:US20180177767A1
公开(公告)日:2018-06-28
Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
Bulky P,PO ligands were designed to inhibit isomerization and reduction side reactions during the crosscoupling between sterically hindered aryl halides and alkylboronic acids. Suzuki–Miyaura cross‐couplings between di‐ortho‐substituted aryl bromides and acyclic secondary alkylboronic acids have been achieved with high yields. The method has also enabled the preparation of ortho‐alkoxy di‐ortho‐substituted