We present herein an unprecedented diastereoconvergent synthesis of vicinal diamines from diols through an economical, redox-neutral process. Under cooperative ruthenium and Lewis acid catalysis, readily available anilines and 1,2-diols (as a mixture of diastereomers) couple to forge two C−N bonds in an efficient and diastereoselective fashion. By identifying an effective chiral iridium/phosphoric
POLYPHENOL COMPOUNDS FOR INHIBITING PROTEASOME AND USES THEREOF
申请人:CHAN Tak-Hang
公开号:US20110152210A1
公开(公告)日:2011-06-23
Synthetic polyphenolic compounds of formula (I), their modes of synthesis, and pharmaceutical compositions thereof are provided herein. Use of the compounds and compositions described herein for inhibiting proteasomal activity and for treating cancer is also provided.
Synthetic polyphenolic compounds of formula (I), their modes of synthesis, and pharmaceutical compositions thereof are provided herein. Use of the compounds and compositions described herein for treating cancer and for treating metabolic disorders is also provided.
Vicinal diols are epoxidised in the presence of a promoter comprising water, aldehyde or ketone using as catalyst the hydroxide, oxide or carboxylates of certain alkali metals supported on amorphous silica.