43083-58-5Relevant academic research and scientific papers
Catalytic Asymmetric Synthesis of anti-α,β-Diamino Acid Derivatives
Izumi, Sanae,Kobayashi, Yusuke,Takemoto, Yoshiji
, p. 696 - 699 (2016/03/01)
A novel approach to chiral anti-α,β-diamino acid derivatives through tandem orthogonal organocatalysis has been developed. Chiral phosphoric acid catalysts control the chemo-, regio-, and stereoselective addition of hydroxylamines to alkylideneoxazolones, while a phosphine catalyst promotes the isomerization of Z- alkylideneoxazolones to the more reactive E- alkylideneoxazolones. (Chemical Equation Presented).
Synthesis, in-vitroreverse transcriptase inhibitory activity and docking study of some new imidazol-5-one analogs
Mokale, Santosh N.,Lokwani, Deepak K.,Shinde, Devanand B.
, p. 3752 - 3764 (2014/08/05)
Non-nucleoside reverse transcriptase inhibitors have a definitive role and most commonly used in treatment of HIV-1 infection. A new series of 4-ethylidene/substituted-benzylidene-1-(4-hydroxy/chloro-6-methylpyrimidin-2-yl) -2-ethyl/phenyl-1H-imidazol-5(4H)-one were designed, synthesized, and evaluated for HIV-1 reverse transcriptase (RT) inhibitory activity. The results of in-vitro HIV-1 RT assay showed that some of the new compounds, such as 4c, 4d, 4e, 5a, and 5e effectively inhibit HIV-1 RT activity. 1-(4-Chloro-6- methylpyrimidin-2-yl)-4-(furan-2-ylmethylene)-2-methyl-1H-imidazol-5(4H)-one (5e) exerted most potent in-vitro HIV-1 RT inhibitory activity, among the group of compounds. Molecular docking studies were carried out to explore the binding affinity of imidazole-5-one analogs in active site of HIV-1 RT enzyme. Springer Science+Business Media 2014.
Synthesis, biological activity and docking study of imidazol-5-one as novel non-nucleoside HIV-1 reverse transcriptase inhibitors
Mokale, Santosh N.,Lokwani, Deepak,Shinde, Devanand B.
experimental part, p. 3119 - 3127 (2012/06/29)
A novel series of substituted imidazol-5-ones were designed, synthesized and evaluated for in vitro reverse transcriptase (RT) inhibition activity using reverse transcriptase assay kit (Roche, Colorimetric). It has been observed from in vitro screening that newly synthesized compounds possess RT inhibitory activity. Docking study was performed to study the binding orientation and affinity of synthesized compounds for RT enzyme.
Thionation of N-acylthreonine and its methyl ester with Lawesson's reagent: Synthesis of 5-oxazolones, 5-thiazolones and thiazolines
Ori, Mayuko,Nishio, Takehiko
, p. 201 - 208 (2007/10/03)
The treatment of N-acylthreonine (1) with Lawesson's reagent [LR: 2,4-bis(p-methoxyphenyl)-1,3,2,4-dithiaphosphetane 2,4-disulfide] afforded 5-oxazolones (2) in moderate yields, along with 5-thiazolones (3). On the other hand, N- acylthreonine methyl este
5(4H)-oxazolones. Part XIII. A new synthesis of 4-ylidene-5(4H)- oxazolones by the Stille reaction
Beccalli, Egle Maria,Clerici, Francesca,Gelmi, Maria Luisa
, p. 781 - 786 (2007/10/03)
4-Chloromethylene-2-phenyl-5(4H)-oxazolone 1 was used as the starting material for the preparation of a series of 4-ylideneoxazolones 3 by the Stille reaction. When compound 1 was reacted with organostannanes 2 in the presence of the palladium catalyst, o
