An efficient and concise strategy for the synthesis of cyclic dipeptides via Pd-catalyzed site-selective δ-C(sp2)–H amination/fluorination and N-to-C cyclization is disclosed. The backbone amides within the dipeptides serves as endogenous directing groups, while the desired products were switched by the C-terminal ester group. This chemistry presents a novel and robust alternative to construct cyclodipeptide
公开了一种通过 Pd 催化的位点选择性 δ-C(sp 2 )–H 胺化/氟化和 N 至 C 环化合成环状二肽的有效且简洁的策略。二肽内的主链酰胺充当内源性导向基团,而所需产物则通过 C 端酯基团进行转换。这种化学方法为构建环二肽片段提供了一种新颖且可靠的替代方案。
COMPOUNDS FOR ENZYME INHIBITION
申请人:Shenk Kevin D.
公开号:US20100144648A1
公开(公告)日:2010-06-10
One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.