63547-22-8Relevant articles and documents
A kind of central nervous system drugs intermediate arab League Qu Feini the synthetic method of the compound of
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Paragraph 0054-0056, (2017/03/17)
The invention relates to a synthesis method of a central nervous system drug adrafinil intermediate compound, namely the synthesis method of a compound expressed by a formula (I) as shown in the specification. According to the synthesis method, a compound expressed by a formula (II) as shown in the specification reacts with a compound expressed by a formula (III) as shown in the specification in an acidic organic solvent in the presence of a catalyst, an organic ligand and an activator to obtain the compound expressed by the formula (I), wherein X is a halogen. Besides, the invention also provides a purification method of the compound expressed by the formula (I); according to the purification method, the target product with extremely high purity can be obtained by virtue of appropriate selection of a recrystallization solvent, a temperature rise rate and a cooling rate.
COMPOSITIONS AND METHODS FOR THE TREATMENT OF NEUROLOGICAL DEGENERATIVE DISORDERS AND NEUROLOGICAL DISEASES
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Paragraph 0106; 0107, (2015/05/26)
The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of neurological degenerative disorders and neurological diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of narcolepsy, shift work sleep disorder, and as an adjunct treatment for obstructive sleep apnea/hypopnea, hypersomnias, like idiopathic hypersomnia, Psychiatric/neurodegenerative disorders, ADHD, Psychiatric/neurodegenerative disorders, Depersonalization disorder, Cognitive enhancement, Fatigue, Post-chemotherapy cognitive impairment and weight loss.
Elucidation of structural elements for selectivity across monoamine transporters: Novel 2-[(diphenylmethyl)sulfinyl]acetamide (modafinil) analogues
Okunola-Bakare, Oluyomi M.,Cao, Jianjing,Kopajtic, Theresa,Katz, Jonathan L.,Loland, Claus J.,Shi, Lei,Newman, Amy Hauck
, p. 1000 - 1013 (2014/03/21)
2-[(Diphenylmethyl)sulfinyl]acetamide (modafinil, (±)-1) is a unique dopamine uptake inhibitor that binds the dopamine transporter (DAT) differently than cocaine and may have potential for the treatment of psychostimulant abuse. To further investigate structural requirements for this divergent binding mode, novel thio- and sulfinylacetamide and ethanamine analogues of (±)-1 were synthesized wherein (1) the diphenyl rings were substituted with methyl, trifluoromethyl, and halogen substituents and (2) substituents were added to the terminal amide/amine nitrogen. Halogen substitution of the diphenyl rings of (±)-1 gave several amide analogues with improved binding affinity for DAT and robust selectivity over the serotonin transporter (SERT), whereas affinity improved at SERT over DAT for the p-halo-substituted amine analogues. Molecular docking studies, using a subset of analogues with DAT and SERT homology models, and functional data obtained with DAT (A480T) and SERT (T497A) mutants defined a role for TM10 in the substrate/inhibitor S1 binding sites of DAT and SERT.
