Synthesis of a TMC-95A ketomethylene analogue by cyclization via intramolecular Suzuki coupling

被引：51

作者：

Kaiser, M

Siciliano, C

Assfalg-Machleidt, I

Groll, M

Milbradt, AG

Moroder, L ^{[1
]}

机构：

[1] AG Bioorgan Chem, Max Planck Inst Biochem, D-82152 Martinsried, Germany

[2] Univ Munich, Adolf Butenandt Inst, D-80336 Munich, Germany

来源：

ORGANIC LETTERS | 2003年 / 5卷 / 19期

关键词：

D O I：

10.1021/ol035178f

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

[GRAPHICS] A TMC-95A analogue extended at the C-terminus with NlePsi[COCH2]Gly-Ala-Ala-NH2 Was synthesized via side-chain cyclization of the linear precursor by a Suzuki cross-coupling reaction in solution to analyze the effect of additional P' residues on the inhibitory potency against yeast proteasome.

引用

页码：3435 / 3437

页数：3