847727-21-3Relevant articles and documents
Engaging sulfinate salts via Ni/photoredox dual catalysis enables facile Csp2-SO2R coupling
Cabrera-Afonso, María Jesús,Lu, Zhi-Peng,Kelly, Christopher B.,Lang, Simon B.,Dykstra, Ryan,Gutierrez, Osvaldo,Molander, Gary A.
, p. 3186 - 3191 (2018/03/30)
This report details the development and implementation of a strategy to construct aryl- and heteroaryl sulfones via Ni/photoredox dual catalysis. Using aryl sulfinate salts, the C-S bond can be forged at room temperature under base-free conditions. An array of aryl- and heteroaryl halides are compatible with this approach. The broad tolerance and mild nature of the described reaction could potentially be employed to prepare sulfones with biological relevance (e.g., in bioconjugation, drug substance synthesis, etc.) as demonstrated in the synthesis of drug-like compounds or their precursors. When paired with existing Ni/photoredox chemistry for Csp3-Csp2 cross-coupling, an array of diverse sulfone scaffolds can be readily assembled from bifunctional electrophiles. A mechanistic manifold consistent with experimental and computational data is presented.
Syntheses, radiolabelings, and in vitro evaluations of fluorinated pet radioligands of 5-HT6 serotoninergic receptors
Colomb, Julie,Becker, Guillaume,Fieux, Sylvain,Zimmer, Luc,Billard, Thierry
supporting information, p. 3884 - 3890 (2014/05/20)
The 5-HT6 receptors are potent therapeutic targets for psychiatric and neurological diseases (schizophrenia, Alzheimers disease, etc.). However, with lack of specific radiopharmaceuticals, their pharmacology is still incomplete and their exploration is limited to animal models. In this context, we have designed a fluorinated PET radiotracer, [18F]2FNQ1P, that possesses a high affinity and selectivity for 5-HT6. In vitro PET autoradiographies in rat brain sections with this radiotracer were in accordance with the 5-HT6 distribution pattern.
COMBINATION OF CB2 LIGAND AND PARACETAMOL
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Page/Page column 190, (2008/12/04)
Combination of one or more CB2 modulators and paracetamol are useful of treating conditions which are mediated by the activity of CB2 receptors such as an immune disorder, an inflammatory disorder, pain, rheumatoid arthritis, multiple sclerosis, osteoarthritis, and osteoporosis.