55427-33-3Relevant articles and documents
Development of a One-Pot Four C-C Bond-Forming Sequence Based on Palladium/Ruthenium Tandem Catalysis
Manick, Anne-Doriane,Berhal, Farouk,Prestat, Guillaume
supporting information, p. 194 - 197 (2018/01/17)
A one-pot four C-C bond-forming sequence has been developed using two distinct transition metal complexes. The sequence entails a double Pd-catalyzed allylic alkylation followed by a Ru-catalyzed ring-closing metathesis and a Pd-catalyzed Heck coupling. The use of various active methylene nucleophiles was examined with yields up to 76% (93% per C-C bond).
Pyrimidine-2,4,6-trione derivatives and their inhibition of mutant SOD1-dependent protein aggregation. Toward a treatment for amyotrophic lateral sclerosis
Xia, Guoyao,Benmohamed, Radhia,Kim, Jinho,Arvanites, Anthony C.,Morimoto, Richard I.,Ferrante, Robert J.,Kirsch, Donald R.,Silverman, Richard B.
experimental part, p. 2409 - 2421 (2011/06/19)
Amyotrophic lateral sclerosis (ALS) is a fatal neurodegenerative disease characterized by the progressive loss of motor neurons, leading to muscle weakness, paralysis, and death, most often from respiratory failure. The only FDA-approved drug for the treatment of ALS, riluzole, only extends the median survival in patients by 2-3 months. There is an urgent need for novel therapeutic strategies for this devastating disease. Using a high-throughput screening assay targeting an ALS cultured cell model (PC12-G93A-YFP cell line), we previously identified three chemotypes that were neuroprotective. We present a further detailed analysis of one promising scaffold from that group, pyrimidine-2,4,6-triones (PYTs), characterizing a number of PYT analogues using SAR and ADME. The PYT compounds show good potency, superior ADME data, low toxicity, brain penetration, and excellent oral bioavailability. Compounds from this series show 100% efficacy in the protection assay with a good correlation in activity between the protection and protein aggregation assays. The modifications of the PYT scaffold presented here suggest that this chemical structure may be a novel drug candidate scaffold for use in clinical trials in ALS.
N,N-Dialkylalloxans - a new class of catalyst for dioxirane epoxidations
Carnell, Andrew J.,Johnstone, Robert A. W.,Parsy, Christophe C.,Sanderson, William R.
, p. 8029 - 8032 (2007/10/03)
N,N-Dimethyl- and N,N-dibenzylalloxans 1a and 1b have been prepared and used as novel dioxirane catalysts for the epoxidation of a range of di- and tri-substituted alkenes in good to excellent yield. The dibenzylalloxan 1b can be recovered in high yield with no evidence of catalyst decomposition.
