- SELECTIVE HDAC1 AND HDAC2 INHIBITORS
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Provided herein are compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1 and/or HDAC2. Such diseases include cancer, sickle-cell anemia, beta-thalassemia, and HIV.
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Paragraph 0376; 0379; 0380
(2014/05/20)
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- Synthesis of Substituted Benzothienopyrazines
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The synthesis of a series of novel 1-unsubstituted and 1-alkyl-1,2,3,4-tetrahydrobenzothienopyrazine-2,3-diones 4a-d and their corresponding dialkylaminoalkylamino derivatives 6a-d starting from 2-nitro-3-bromobenzothiophene is described.The
- Cannizzo, Sergio,Guerrera, Francesco,Siracusa, Maria Angela,Corsaro, Antonino
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p. 2175 - 2179
(2007/10/02)
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- Bromonitromethane. A Versatile Electrophile
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Pathways in reactions of bromonitromethane with a variety of nucleophiles have been investigated.With thiolates, the electrophilic centre is bromine and the initial products are disulphides.When the thiolate ion itself carries an electrophilic centre such as carbonyl or cyano β-to sulphur, the product is a nitrothiophene derived from subsequent reaction of the first-formed disulphide with nitronate ion displaced in the initial process.This provides a generalisation of earlier nitrothiophene synthesis by this route.In reactions with arenesulphinate ion, the electrophilic centre is also bromine and equilibration between the initial reactants and the initial products, sulphonyl bromide and nitronate ion, is established.The components of the equilibrium subsequently react either with each other or with the solvent.Reactions with sulphides are slow and distal substituents such as hydroxy- or cyano- so much reduce reactivity that no reaction is observed.Dimethyl sulfide attacks bromonitromethane at the carbon atom,and subsequent attack on the nitromethyl sulphonium salt initially formed gives methylthionitromethane and trimethylsulphonium bromide.Iodide ion attacks at bromine to give iodine, presumably via iodine bromide, but with tervalent phosphorus nucleophiles, attack is at oxygen giving the corresponding oxides and HCN in a double deoxygenation sequence.For hydroxide, methoxide and hydride ions (from sodium borohydride), nucleophilic attack is at hydrogen and the nitronate ion produced is inert to further attack.There is no evidence of carbene formation by α-elimination.When the anion of bromonitromethane is allowed to react with tributylboron, the anionic migration-displacement which follows boron-carbon bond formation, yields 1-nitropentane.The anion of bromonitromethane is unreactive towards aldehydes and electrophilic alkenes.
- Fishwick, Brian R.,Rowles, David K.,Stirling, Charles J. M.
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p. 1171 - 1180
(2007/10/02)
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- Bromonitromethane, a Versatile Electrophile: Reactions with Thiolates
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Thiolate ions react with bromonitromethane to give nitronate ion and, initially, sulphenyl bromide which reacts with further thiolate ion to give disulphide; when the disulphide bears an appropriately placed nitrile function, intramolecular attack by the nitronate ion at this function and subsequent intramolecular displacement of thiolate ion yields aminothiophenes.
- Fishwick, Brian R.,Rowles, David K.,Stirling, Charles J. M.
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p. 834 - 835
(2007/10/02)
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