2351-88-4Relevant academic research and scientific papers
TARGETING GLI PROTEINS IN HUMAN CANCER BY SMALL MOLECULES
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Paragraph 00239, (2014/08/07)
The present disclosure provides compositions, pharmaceutical preparations and methods for the diagnosis and treatment of cancers expressing a GLI polypeptide. The disclosed compositions and pharmaceutical preparations may comprise one or more pyrazolyl-containing compounds, or an analog or derivative thereof.
TARGETING GLI PROTEINS IN HUMAN CANCER BY SMALL MOLECULES
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Paragraph 00228, (2013/03/26)
The present disclosure provides compositions, pharmaceutical preparations and methods for the diagnosis and treatment of cancers expressing a GLI polypeptide. The disclosed compositions and pharmaceutical preparations may comprise one or more pyrazolyl-containing compounds, or an analog or derivative thereof.
A practical, efficient, and atom economic alternative to the Wittig and Horner-Wadsworth-Emmons reactions for the synthesis of (E)-α,β- unsaturated esters from aldehydes
List, Benjamin,Doehring, Arno,Hechavarria Fonseca, Maria T.,Job, Andreas,Rios Torres, Ramon
, p. 476 - 482 (2007/10/03)
We describe a highly efficient new methodology for the synthesis of (E)-α,β-unsaturated esters from aldehydes. In our DMAP-catalyzed reaction, both aromatic as well as aliphatic aldehydes furnish the desired products highly regio- and stereoselectively if treated with commercially available or synthetically easily accessible malonic acid half ester. A large scale application in the synthesis of p-methoxycinnamates, which are of use as sunscreen ingredients, is described.
A simple one-pot organometallic formylation/trapping sequence using N-formylcarbazole
Dixon, Darren J.,Lucas, Amanda C.
, p. 1092 - 1094 (2007/10/03)
Treatment of a range of sp3-, sp2- and sp-nucleophiles with N-formyl carbazole leads to the formation of the metastable anionic carbazole carbinols. In the presence of a second nucleophilic reagent such as phosphonoacetate or an organolithium, these collapse on warming to the aldehyde which is trapped in situ to afford the α,β-unsaturated esters or secondary carbinols respectively.
In situ oxidative diol cleavage - Wittig processes
Outram, Helen S.,Raw, Steven A.,Taylor, Richard J.K.
, p. 6185 - 6187 (2007/10/03)
1,2-Diol cleavage followed by in situ trapping of the resulting aldehyde with a stabilised phosphorane is described; both manganese dioxide and silica-supported sodium periodate can be used as the heterogeneous oxidant, but the latter reagent is generally the most efficient.
Base-Catalyzed Reactions of α,β-Unsaturated Esters and Nitriles. 4. Dimerization of β-Alkyl-Substituted Acrylates
Shabtai, Joseph,Ney-Igner, Eva
, p. 3795 - 3802 (2007/10/02)
2-Butenoates 1-C4 alkyl, cyclohexyl, or 1-bornyl> and higher β-alkyl-substituted acrylates 2-C9 n-alkyl> undergo highly selective (>95percent) dimerization in the presence of promoted potassium or sodium catalysts to yield corresponding 2-alkylidene-3-alkylglutarates (3).The reaction involves metalation of the β-alkylacrylate at the C-2 position, followed by addition at C-3 of a second monomeric molecule.Changes in the relative extent of dimerization (Kr) as a function of structural and experimentalvariables were determined.Kr is strongly dependent upon the inductive and steric characteristics of the alcoholic (R) group and of the β-alkyl substituent (R').For an n-alkyl group as R' the Kr value increases with increase in chain length from C1 to C4 but then decreases for longer substituents (C5-C9).Among the two geometric isomers in the dimeric product 3, the isomer with an α-vinylic hydrogen cis to the carboalkoxy group is predominant in all cases, but its relative concetration decreases with an increase in the size of R'.Branched or cyclic β-substituents in 2 prevent dimerization due to steric hindrance in the rate-determining addition step.Promoted potassium or sodium catalysts show much higher dimerization activity compared to supported alkali metals or to alkoxides.For conversions of up to 60percent, Kr values in proton-exchanging alkylbenzene solvents and in nonexchanging alkylcyclohexanes are closely similar, indicating faster abstraction of an α-vinylic hydrogen from the monomer, rather than a benzylic hydrogen from the solvent, in the chain regeneration step of the reaction.
A SIMPLE SYNTHESIS OF α,β-UNSATURATED CARBONYL COMPOUNDS BY TRAPPING THE MICHAEL ADDITION-ENOLATE ANION WITH METHANESULFINYL CHLORIDE
Fujisawa, Tamotsu,Noda, Atsunari,Kawara, Tatsuo,Sato, Toshio
, p. 1159 - 1160 (2007/10/02)
Trapping of an enolate anion, formed by the Michael addition, with methanesulfinyl chloride and subsequent desulfinylation is found to be a useful method for the synthesis of various α,β-unsaturated carbonyl compounds.Synthetic utility of this method is demonstrated in the synthesis of geraniol, nerol, farnesol, and dihydrojasmone.
