75889-54-2Relevant academic research and scientific papers
CO2-Catalyzed oxidation of benzylic and allylic alcohols with DMSO
Riemer, Daniel,Mandaviya, Bhavdip,Schilling, Waldemar,G?tz, Anne Charlotte,Kühl, Torben,Finger, Markus,Das, Shoubhik
, p. 3030 - 3034 (2018/04/14)
CO2-catalyzed transition-metal-free oxidation of alcohols has been achieved. Earlier, several methodologies have been explored for alcohol oxidations based on transition-metal catalysts. However, owing to the cheaper price, easy separation and nontoxicity, transition-metal-free systems are in high demand to the pharmaceutical industries. For this reason, various primary and secondary alcohols have been selectively oxidized to the corresponding carbonyl compounds using CO2 as a catalyst in the presence of different functional groups such as nitrile, nitro, aldehyde, ester, halogen, ether, and so on. At the end, transition-metal-free syntheses of pharmaceuticals have also been achieved. Finally, the role of CO2 has been investigated in detail, and the mechanism is proposed on the basis of experiments and DFT calculations.
Stereoselective synthesis of trans-dihydronarciclasine derivatives containing a 1,4-benzodioxane moiety
Varró, Gábor,Pogrányi, Balázs,Grün, Alajos,Simon, András,Heged?s, László,Kádas, István
, p. 2265 - 2285 (2018/11/10)
Abstract: Some new trans-dihydronarciclasine derivatives containing a 1,4-benzodioxane moiety were stereoselectively synthesised using our feasible and efficient method developed recently. These new phenanthridone alkaloid analogues were obtained in both racemic and optically active forms. High enantioselectivities (up to 99% ee) were achieved by applying (8S,9S)-9-amino(9-deoxy)epiquinine as an organocatalyst. Due to a side reaction, various methoxyphenanthridine regioisomers were also prepared which afforded further synthetic trans-dihydronarciclasine analogues modified in the ring A of the phenanthridone scaffold. Graphical abstract: [Figure not available: see fulltext.].
Cis -restricted 3-aminopyrazole analogues of combretastatins: Synthesis from plant polyalkoxybenzenes and biological evaluation in the cytotoxicity and phenotypic sea urchin embryo assays
Tsyganov, Dmitry V.,Konyushkin, Leonid D.,Karmanova, Irina B.,Firgang, Sergei I.,Strelenko, Yuri A.,Semenova, Marina N.,Kiselyov, Alex S.,Semenov, Victor V.
, p. 1485 - 1491 (2013/09/23)
We have synthesized a series of novel cis-restricted 4,5-polyalkoxydiaryl- 3-aminopyrazole analogues of combretastatins via short synthetic sequences using building blocks isolated from dill and parsley seed extracts. The resulting compounds were tested in vivo in the phenotypic sea urchin embryo assay to reveal their antimitotic and antitubulin effects. The most potent aminopyrazole, 14a, altered embryonic cell division at 10 nM concentration, exhibiting microtubule-destabilizing properties. Compounds 12a and 14a displayed pronounced cytotoxicity in the NCI60 anticancer drug screen, with the ability to inhibit growth of multi-drug-resistant cancer cells.
Synthesis and glycogen phosphorylase inhibitor activity of functionalized 1,4-benzodioxanes
Czako,Juhasz,Docsa,Gergely,Antus
experimental part, p. 235 - 238 (2011/07/09)
A series of novel 1,4-benzodioxanes 11a-e and rac-12a-d carrying thiazolidine-2,4-dione moiety was synthesized and their glycogen phosphorylase inhibitor activity was also evaluated.
Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
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, (2008/06/13)
The present invention provide a compound of formula I or II: or a pharmaceutically acceptable derivative thereof, wherein R1, R2, R3, and R4 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli; and Src-family kinases, especially Src and Lck kinases. These compounds are also inhibitors of GSK3 and CDK2 kinases. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
