260270-95-9Relevant academic research and scientific papers
Enantioselective and Diastereodivergent Access to α-Substituted α-Amino Acids via Dual Iridium and Copper Catalysis
Zhang, Jiacheng,Huo, Xiaohong,Li, Bowen,Chen, Zhouli,Zou, Yashi,Sun, Zhenliang,Zhang, Wanbin
, p. 1130 - 1139 (2019)
The work reported within this paper describes an example of the application of bimetallic catalysts system in allylic substitution reactions. The development of new nucleophiles and the control of enantio- and diastereoselectivity are the main research topics in this area. An improvement in the reactivity and diastereoselectivity has been realized for the dual Ir/Cu catalyzed allylic alkylation of inactive prochiral nucleophiles, under mild reaction conditions. Furthermore, the choice of the metallacyclic iridium complex and chiral Cu-Phox complex combination allows for access to all four stereoisomers from the same starting materials with excellent enantioselectivity and diastereoselectivity (up to >99% ee and >20:1 dr). Significantly, this method provides a stereodivergent access to 2-amino-3-methylpent-4-acid ester, an important fragment for the synthesis of Halipeptin A. (Figure presented.).
With chiral 3 - substituted 3 - vinyl -2 - alkylamino propionate and its preparation method (by machine translation)
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Paragraph 0217-0221, (2019/04/06)
The present invention has offered a kind of chiral 3 - substituted 3 - vinyl - 2 - alkylamino propionate, structural formula as follows: The invention also provides the above-mentioned synthetic 3 - substituted 3 - vinyl - 2 - alkylamino propionate method, its reaction as follows: The invention has strong substrate serviceability, mild reaction conditions, the operation is simple, the cost of synthesizing low and the like, only needs one-step reaction can be realized continuous chiral center has the 3 - substituted 3 - vinyl - 2 - alkylamino propionate three-dimensional divergent synthesis. The product of this invention can be directly applied with strong anti-sars activity to the marine natural product Hal ipeptin A important chiral amino acid fragment into selective synthesis, the original process is greatly shortened. (by machine translation)
Design of selective and soluble inhibitors of tumor necrosis factor-α converting enzyme (TACE)
Rabinowitz,Andrews,Becherer,Bickett,Bubacz,Conway,Cowan,Gaul,Glennon,Lambert,Leesnitzer,McDougald,Moss,Musso,Rizzolio
, p. 4252 - 4267 (2007/10/03)
A program to improve upon the in vitro, in vivo, and physicochemical properties of N-hydroxyformamide TACE inhibitor GW 3333 (1) is described. Using the primary structure of pro-TNF-α, along with a homology model of the catalytic domain of TACE based on t
Formamide compounds as therapeutic agents
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, (2008/06/13)
A family of compounds having the general structural formula where W is a reverse hydroxamic acid group, and R1, R2, R3, R4, R5and R6are as described in the specification, or a pharmaceutica
