1219424-59-5Relevant articles and documents
Discovery of an Orally Active Small-Molecule Tumor Necrosis Factor-α Inhibitor
Sun, Weiguang,Wu, Yanli,Zheng, Mengzhu,Yang, Yueying,Liu, Yang,Wu, Canrong,Zhou, Yirong,Zhang, Yonghui,Chen, Lixia,Li, Hua
, p. 8146 - 8156 (2020)
Tumor necrosis factor α (TNF-α) is an important therapeutic target for rheumatoid arthritis, inflammatory bowel disease, and septic hepatitis. In this study, structure-based virtual ligand screening combined with in vitro and in vivo assays were applied.
Chemo-enzymatic preparation of chiral 3-aminopyrrolidine derivatives
Iding, Hans,Wirz, Beat,Rogers-Evans, Mark
, p. 647 - 653 (2007/10/03)
A new simple method for the enantioselective enzymatic hydrolysis of N-protected D-asparagine esters suitable for the use on the preparative scale is presented. Due to major obstacles observed under conventional reaction conditions - racemization of the retained ester and a strong enzyme inactivation - a comparatively low pH together with an organic co-solvent had to be employed. Under these conditions, nearly all tested proteases demonstrated good activity and excellent enantioselectivity giving access to the corresponding D-esters and L-asparagines in high optical purities (>95% ee) and good chemical yields (>40%). From the unnatural D-asparagine derivative, sequential cyclization, selective deprotection and reduction yielded efficiently benzyl protected (R)-3-aminopyrrolidine, a homo-chiral building block utilized in numerous drug candidates.
Process for producing 1H-3-aminopyrrolidine and derivatives thereof
-
, (2008/06/13)
A process for producing 1H-3-aminopyrrolidine and derivatives thereof is disclosed. The process is especially useful for producing optically active 1H-3-aminopyrrolidine and derivatives thereof and in this case comprises reacting an optically active amino