On May 31, 2018, Zhang, Xuekai; Lu, Gang; Sun, Meng; Mahankali, Madhu; Ma, Yanfei; Zhang, Mingming; Hua, Wangde; Hu, Yuting; Wang, Qingbing; Chen, Jinghuo; He, Gang; Qi, Xiangbing; Shen, Weijun; Liu, Peng; Chen, Gong published an article.Reference of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate The title of the article was A general strategy for synthesis of cyclophane-braced peptide macrocycles via palladium-catalyzed intramolecular sp3 C-H arylation. And the article contained the following:
New methods capable of effecting cyclization, and forming novel three-dimensional structures while maintaining favorable physicochem. properties are needed to facilitate the development of cyclic peptide-based drugs that can engage challenging biol. targets, such as protein-protein interactions. Here, we report a highly efficient and generally applicable strategy for constructing new types of peptide macrocycles using palladium-catalyzed intramol. C(sp3)-H arylation reactions. Easily accessible linear peptide precursors of simple and versatile design can be selectively cyclized at the side chains of either aromatic or modified non-aromatic amino acid units to form various cyclophane-braced peptide cycles. This strategy provides a powerful tool to address the long-standing challenge of size- and composition-dependence in peptide macrocyclization, and generates novel peptide macrocycles with uniquely buttressed backbones and distinct loop-type three-dimensional structures. Preliminary cell proliferation screening of the pilot library revealed a potent lead compound with selective cytotoxicity toward proliferative Myc-dependent cancer cell lines. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Reference of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate
The Article related to cyclodepsipeptide cyclophane diastereoselective synthesis antitumor structure activity crystal structure, arylation palladium catalyst transition state ring strain energy dft, amino acid iodination esterification peptide coupling solid phase synthesis and other aspects.Reference of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics