strategy for constructing diverse peptide structural architectures via chemoselective peptideligation. The key advancement involved is to utilize the benzofuran moiety as the peptide salicylaldehyde ester surrogate, and Dap–Ser/Lys–Ser dipeptide as the hydroxyl amino functionality, which could be successfully introduced at the side chain of peptides enabling peptideligation. With this method, the side
在此,我们报告了一种通过化学选择性肽连接构建不同肽结构的简便合成策略的发展。所涉及的关键进展是利用苯并呋喃部分作为肽水杨醛酯替代物,以及Dap-Ser/Lys-Ser二肽作为羟基氨基官能团,可以成功地将其引入到肽的侧链上,从而实现肽连接。通过该方法,设计并成功合成了侧链至侧链环肽、支链/桥接肽、带尾环肽和多环肽,并在连接位点成功合成了天然肽键。这一战略为合成肽的发展提供了另一种战略机遇。它还为新模式的 PPI 抑制剂的结构设计提供了灵感。
US7985860B2
申请人:——
公开号:US7985860B2
公开(公告)日:2011-07-26
[EN] PROCESS AND INTERMEDIATES FOR THE SYNTHESIS OF 2-(QUINOLIN-5-YL)-4,5 DISUBSTITUTED-AZOLE DERIVATIVES<br/>[FR] PROCÉDÉ ET INTERMÉDIAIRES DE SYNTHÈSE DE DÉRIVÉS D'AZOLE 2-(QUINOLIN-5-YL)-4,5-DISUBSTITUÉS
申请人:SCHERING CORP
公开号:WO2008021235A2
公开(公告)日:2008-02-21
[EN] This application discloses a novel process to synthesize 2-(Quinolin-5yo)-4,5-Disubstituted-Azole derivatives, which may be used, for example, as PDE IV inhibitor compounds in pharmaceutical preparations. [FR] La présente demande a pour objet un nouveau procédé de synthèse de dérivés d'azole 2-(quinolin-5-yl)-4,5-disubstitués, qui peuvent être par exemple employés en tant que composés inhibiteurs de PDE IV dans des préparations pharmaceutiques.
Process and intermediates for the synthesis of 2-(quinolin-5-yl)-4,5 disubstituted-azole derivatives
申请人:Cutarelli D. Timothy
公开号:US20080045718A1
公开(公告)日:2008-02-21
This application discloses a novel process to synthesize 2-(Quinolin-5yo)-4,5-Disubstituted-Azole derivatives, which may be used, for example, as PDE IV inhibitor compounds in pharmaceutical preparations.