691889-37-9Relevant academic research and scientific papers
BIPHENYL DERIVATIVES AS MODULATORS OF THE HISTAMINE-H3 RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
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Page/Page column 56-57, (2009/06/27)
Biphenyl derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the H3 histamine receptor. (Ia) Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders, such as cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness, such as narcolepsy, shift-work syndrome, drowsiness as a side effect from a medication, maintenance of vigilance to aid in completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, dementia, Alzheimer's disease, pain and the like.
Parallel kinetic resolution of active esters using designer oxazolidin-2-ones derived from phenylglycine
Chavda, Sameer,Coulbeck, Elliot,Dingjan, Marco,Eames, Jason,Flinn, Anthony,Northen, Julian
, p. 1536 - 1548 (2008/12/21)
The parallel kinetic resolution of racemic pentafluorophenyl 2-phenylpropionate using an equimolar combination of quasi-enantiomeric oxazolidin-2-ones is discussed. The levels of diastereoselectivity were excellent (>90% de) leading to separable quasi-enantiomeric oxazolidin-2-one adducts in good yield. This methodology was subsequently used to resolve a series of 2-aryl propionic and butanoic acids.
A Reactivity/Affinity Switch for Parallel Kinetic Resolution: α-Amino Acid Quasienantiomers and the Resolution of Cyclopropene Carboxylic Acids
Liao, Lian-An,Zhang, Fan,Dmitrenko, Olga,Bach, Robert D.,Fox, Joseph M.
, p. 4490 - 4491 (2007/10/03)
A new type of parallel kinetic resolution (PKR) is reported in which quasienantiomers with very similar reactivities give products whose chromatographic properties diverge upon the addition of fluoride. This concept of a reactivity/affinity switch is applied to the PKR of cyclopropene carboxylic acids with all-carbon quaternary centers. This is the first application of α-amino acid quasienantiomers in PKR, and it is a complementary approach for acyltransfer systems where the asymmetry is induced by the nucleophile rather than the leaving group. Excellent diastereoselectivities (ranging from 90:10 to 99.5:5) and good yields were obtained for both quasienantiomeric products, and the reactions can be run on significant scale because the separation is trivial. High-level DFT calculations (B3LYP functional with the 6-31+G(d,p) basis set) provided transition-state structures with relative energies that are in accord with the experimental observations. Copyright
