77124-22-2Relevant academic research and scientific papers
COMPOUNDS USEFUL AS MODULATORS OF TRPM8
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Paragraph 0849; 0850, (2016/03/29)
The present invention includes compounds useful as modulators of TRPM8, such as compounds of Formulae (Ia), (Ib) and (Ic), and the subgenus and species thereof; personal products containing those compounds; and the use of those compounds and the personal products, particularly the use of increasing or inducing chemesthetic sensations, such as cooling or cold sensations.
Synthesis and biological evaluation of cycloalkylidene carboxylic acids as novel effectors of Ras/Raf interaction
Friese, Anke,Hell-Momeni, Katja,Zündorf, Ilse,Winckler, Thomas,Dingermann, Theodor,Dannhardt, Gerd
, p. 1535 - 1542 (2007/10/03)
The protooncogenes Ras and Raf play important roles in signal transduction pathways regulated by mitogen-activated protein kinases. Mutations of Ras that arrest the protein in its active state are frequently implicated in tumor formation. We used Ras and Raf proteins in the yeast two-hybrid system to search for natural or synthesized substances capable of modulating Ras/Raf interaction by specifically binding to one of the interacting partners. We found that cycloalkylidene carboxylic acids enhanced Ras/Raf interaction by acting on the cysteine-rich domain of Raf. Several analogues of the active substance 2-cyclohexylidene propanoic acid were synthesized and the importance of the semicyclic double bond in the stabilization of Ras/Raf interaction was demonstrated. Variation of the size and the substituents of the cyclic system as well as the length of the carboxylic acid resulted in enhanced Ras/Raf interaction.
Synthesis of α-Methylene β-Lactones, Novel Heterocycles
Adam, Waldemar,Albert, Rainer,Grau, Nuria Dachs,Hasemann, Ludwig,Nestler, Bernd,et al.
, p. 5778 - 5781 (2007/10/02)
Triphenylphosphin deoxygenation of β-alkyl-, β,β-dialkyl-, and β,β-spirocycloalkyl-substituted α-methylene-β-peroxy lactones 3a-k, which are readily available by photooxygenation of the corresponding α,β-unsaturated carboxylic acids 1, and cyclization of the resulting α-methylene-β-hydroperoxy acids 2 constitute a convenient method for the preparation of a variety of α-methylene β-lactones 5.Alternatively, the α-methylene-β-hydroxycarboxylic acids 4 can be directly cyclized by benzenesulfonyl chloride in pyridine into these novel four membered ring heterocycles 5.
A Simple and Efficient Route to 2-Alkyl-2-alkenoic Acids and 2-Phenyl-2-Alkenoic Acids by the Horner Synthesis. Application to the Steroselective Synthesis of the Pheromone Manicone
Coutrot, Philippe,Ghribi, Abdellaziz
, p. 790 - 792 (2007/10/02)
A general synthesis of α-branched α,β-unsaturated carboxylic acids is described.A Horner reaction of 2-diethoxyphosphorylalkanoic acid dianions (lithium α-lithiocarboxylates) with carbonyl compounds is used.The reaction is applied to the stereoselective synthesis of Manicone.
Phosphite-Mediated in Situ Carboxyvinylation: A New General Acrylic Acid Synthesis
Brittelli, David R.
, p. 2514 - 2520 (2007/10/02)
Sequential treatment of a 2-halo carboxylic acid with a dialkyl phosphite and an aldehyde or ketone in the presence of 3 equiv of sodium hydride in glyme constitutes a new general acrylic acid synthesis superior to conventional methods.An alkoxide-in-alcohol variant may be used with bromo- or chloroacetic acid and aryl aldehydes to produce cinnamic acids conveniently.The scope and other features of the synthesis are discussed.
