- An improved synthesis of substituted benzo[b]thiophenes using microwave irradiation
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An easy and high-yielding method for the synthesis of substituted benzo[b]thiophenes using microwave irradiation is described.
- Allen, Daniel,Callaghan, Owen,Cordier, Frederic L.,Dobson, David R.,Harris, John R.,Hotten, Terry M.,Owton, W. Martin,Rathmell, Richard E.,Wood, Virginia A.
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- Dihydroimidazo[2,1-b]thiazole and dihydro-5h-thiazolo[3,2-A]pyrimidines as antidepressant agents
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The present invention relates to certain novel substituted dihydroimidazo[2,1-b]thiazole and dihydro-5H-thiazolo[3,2-a]pyrimidine compounds of Formula (I) including pharmaceutically acceptable salts thereof in which have affinity for 5-HT1A receptors and which inhibits neuronal reuptake of 5-hydroxytryptamine and/or noradrenaline, to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, obesity, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders such as bulimia, anorexia, snacking and binge eating, non-insulin dependent diabetes mellitus, hyperglycaemia, hyperlipidaemia, stress, as an aid to smoking cessation and in the treatment and/or prophylaxis of seizures, neurological disorders such as epilepsy and/or in which there is neurological damage such as stroke, brain trauma, cerebral ischaemia, head injuries and haemorrhage.
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- N-ALKOXYALKYL-N,N-DIALKYLAMINE DERIVATIVES OR SALTS THEREOF, AND REMEDIES FOR NERVE DEGENERATION DISEASES CONTAINING THE SAME
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An N-alkoxyalkyl-N,N-dialkylamine derivative represented by the following general formula [1]: wherein the ring D represents a 5- or 6-membered heterocyclic ring or hydrocarbon ring; R3 and R4, which are the same or different, represent an unsubstituted or substituted alkyl, cycloalkyl or aralkyl group; and R1, R2, R5, R6, R7, R8, m and n are as defined in the specification, or a salt thereof has an anti-hypoxic activity, a nerve-protecting activity and a nerve regeneration promoting activity and is useful for the treatment of neurodegenerative diseases.
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Example 16'(2)
(2008/06/13)
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- An improved synthesis of benzo[b]thiophene and its derivatives using modified montmorillonite clay catalysts
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Methods for the preparation of benzothiophene (3) and its derivatives by cyclization of phenylthioacetals (1) over ZnCl2-promoted montmorillonite clay are described. Reactions in solution resulted in only moderate (ca. 50%) yields of 3 and the formation of diphenyl disulfide (4) and uncharacterized products. The production of 4 was explained by coordination of 1 via its oxygen atom to active sites of the catalyst and subsequent bimolecular processes. Good to excellent yields (67-98%) of 3 and its derivatives were obtained using vapor phase techniques at 200-300°C to promote the desired intramolecular cyclizations.
- Clark,Kirk,Yee
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p. 1936 - 1938
(2007/10/02)
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- ALKYLATION OF THIOPHENES AND PREPARATION OF BENZOTHIOPHENES USING MODIFIED MONTMORILLONITE CLAY CATALYSTS
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Regioselective benzylation of thiophene and benzothiophene using benzyl chloride and a ZnCl2-promoted montmorillonite catalysts is described.An improved process for the cyclization of (arylthio)acetaldehyde dialkyl acetals to benzothiophenes using the same catalyst is also documented.
- Clark, Peter D.,Kirk, Andrew,Mesher, Shaun T.,Yee, James G.K.
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p. 441 - 444
(2007/10/02)
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- Thermolysis of Thiophenedicarboxylic Acid Anhydrides as a Route to Five-Membered Hetarynes
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Flow vacuum thermolysis (FVT) of the anhydrides of thiophene-2,3- (5) and -3,4-dicarboxylic acid (6) and of thianaphthene-2,3-dicarboxylic acid (7) in the presence of thiophene, 1,3-cyclohexadiene, or benzene gave thianthrene (15a), presumably by aromatization of an intermadiate Diels-Alder adduct of the diene traps and the aryne 2,3-didehydrothiophene (8).A similar rationale explains the formation of dibenzothiophene from 7 and thiophene, the four monomethylthianaphthenes 22-25 from 5 and cyclopentadiene, 5,6-dimethylthianaphthene (15f) from 5 and 2,3-dimethylbutadiene, and a mixture of hydroxythianaphthenes (15d) from 5 and furan.The latter reaction also produces a mixture of isomeric cyclopentanothiophenes (19) which probably arise by decarbonylation of 15d.An FVT reaction of 5 with propyne as the trap gave a mixture of allenyl-(28) and propynylthiophenes 29 which probably arise by an ene reaction of the trap and the aryne 8.Decomposition of the anhydrides 5 and 6 in molten anthracene led only to Friedel-Crafts products such as thienylanthracenes 33 and quinones 34 from 5 and 39 and 40 from 6.The diene reactivity of thiophene 13a in the gas phase was demonstrated by the formation of naphthalene from its reaction with benzyne generated from the thermolysis of indanetrione and by the formation of indene from 13a plus cyclopentadiene.Possible, but improbable, interpretations of the FVT results without invoking a five-membered hetaryne intermediate are considered.
- Reinecke, Manfred G.,Newsom, James G.,Chen, Lao-Jer
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p. 2760 - 2769
(2007/10/02)
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