959508-79-3Relevant academic research and scientific papers
Design and synthesis of new bidentate alkoxy-NHC ligands for enantioselective copper-catalyzed conjugate addition
Clavier, Hervé,Coutable, Ludovic,Toupet, Lo?c,Guillemin, Jean-Claude,Mauduit, Marc
, p. 5237 - 5254 (2005)
A new family of chiral alkoxy-N-heterocyclic carbene (NHC) ligands has been designed for the enantioselective copper-catalyzed conjugate addition of dialkylzincs to enones. These new bidentate NHC ligands were synthesized in high overall yields using a five-step procedure starting from commercially available β-aminoalcohols. Influence of the temperature, base, solvent and copper source were studied in order to optimize the stereoselectivity of the addition. High reactivity and excellent enantioselectivity were obtained at ambient temperature with a range of cyclic enones and dialkylzinc. Addition to acyclic enones has also been studied.
Structure-activity relationship study of a series of caspase inhibitors containing γ-amino acid moiety for treatment of cholestatic liver disease
Mou, Jianfeng,Wu, Songliang,Luo, Zhi,Guo, Fengying,He, Haiying,Wang, Jianhua,Lin, Fusen,Guo, Fengxun,Sun, Jianping,Shen, Liang,Zeng, Minggao,Wang, Chuan,Xu, Deming,Gu, Zhengxian,Tian, Xin,Zhang, Aiming,Xu, Hongjiang,Yang, Ling,Zhang, Xiquan,Li, Jian,Chen, Shuhui
supporting information, p. 1874 - 1878 (2018/04/12)
A series of caspase inhibitors containing γ-amino acid moiety have been synthesized. A systemic study on their structure-activity relationship of anti-apoptotic cellular activity is presented. These efforts led to the discovery of compound 20o as a potent caspase inhibitor, which demonstrated preclinical ameliorating total bilirubin efficacy with a significantly improved pharmacokinetic profile.
