通过分子内铃木偶联环化反应合成TMC-95A酮亚甲基类似物。
Synthesis of a TMC-95A ketomethylene analogue by cyclization via intramolecular Suzuki coupling.
作者信息
Kaiser Markus, Siciliano Carlo, Assfalg-Machleidt Irmgard, Groll Michael, Milbradt Alexander G, Moroder Luis
机构信息
Max-Planck-Institut für Biochemie, AG Bioorganische Chemie, 82152 Martinsried, Germany.
出版信息
Org Lett. 2003 Sep 18;5(19):3435-7. doi: 10.1021/ol035178f.
PMID:12967293
Abstract
[structure: see text] A TMC-95A analogue extended at the C-terminus with NlePsi[COCH(2)]Gly-Ala-Ala-NH(2) 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.
摘要
[结构：见正文] 通过溶液中的铃木交叉偶联反应，对线性前体进行侧链环化，合成了一种在C端延伸有NlePsi[COCH(2)]Gly-Ala-Ala-NH(2)的TMC-95A类似物，以分析额外P'残基对酵母蛋白酶体抑制效力的影响。
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