- FUSED PYRROLIDINE 1,2,4-TRIAZOLE DERIVATIVES AS MODULATORS OF MGLUR5
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The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
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Page/Page column 22
(2009/05/29)
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- AMINO 1,2,4-TRIAZOLE DERIVATIVES AS MODULATORS OF MGLUR5
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The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
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Page/Page column 23-24
(2009/05/29)
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- 1,2,3-TRIAZOLE PYRROLIDINE DERIVATIVES AS MODULATORS OF MGLUR5
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The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
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Page/Page column 10
(2009/05/29)
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- THIOPHENE 1,2,4-TRIAZOLE DERIVATIVES AS MODULATORS OF MGLUR5
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The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
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Page/Page column 19
(2009/05/29)
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- Synthesis of substituted pyridines and pyridazines via ring closing metathesis
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RCM can be used to make aromatic heterocycles, namely pyridines and, for the first time, pyridazines; the key step after RCM involves elimination of sulfinate to provide the aromatic system. The Royal Society of Chemistry 2009.
- Donohoe, Timothy J.,Fishlock, Lisa P.,Basutto, Jose A.,Bower, John F.,Procopiou, Panayiotis A.,Thompson, Amber L.
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supporting information; experimental part
p. 3008 - 3010
(2009/12/01)
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- Ring-closing metathesis for the synthesis of heteroaromatics: evaluating routes to pyridines and pyridazines
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Ring-closing olefin metathesis (RCM) has been applied to the efficient synthesis of densely and diversely substituted pyridine and pyridazine frameworks. Routes to suitable metathesis precursors have been investigated and the scope of the metathesis step has been probed. The metathesis products function as precursors to the target heteroaromatic structures via elimination of a suitable leaving group, which also facilitates earlier steps by serving as a protecting group at nitrogen. Further functionalisation of the metathesis products is possible both prior to and after aromatisation. The net result is a powerful strategy for the de novo synthesis of highly substituted heteroaromatic scaffolds.
- Donohoe, Timothy J.,Bower, John F.,Basutto, José A.,Fishlock, Lisa P.,Procopiou, Panayiotis A.,Callens, Cedric K.A.
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experimental part
p. 8969 - 8980
(2009/12/26)
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- MGLUR5 MODULATORS
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The present invention is directed to compounds of formula (I) Wherein R1 to R5, X and Z are further defined in the description. The invention also relates to processes for the preparation of the compounds and to intermediates used in
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Page/Page column 54
(2008/06/13)
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- MGluR5 modulators I
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The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
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Page/Page column 30
(2008/06/13)
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- MGluR5 modulators V
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The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
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Page/Page column 31
(2008/06/13)
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- The Reaction of Meldrum's Acid with α-Dicarbonyl Monohydrazones: A New Synthesis of Pyridazin-3-ones
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Treatment of the monohydrazones of α-dicarbonyl compounds with Meldrum's acid gives the condensation products (13)-(19) under standard conditions.Reaction of pyruvaldehyde 2-phenylhydrazone or 2-t-butylhydrazone with Meldrum's acid at 80 deg C gives the corresponding 2-substituted-2,3-dihydro-6-methyl-3-oxo-pyridazine-4-carboxylic acids (29) and (30).Cyclisation of the other N-monosubstituted condensation products (13), (14), (16), (18), and (19) to 3-oxopyridazine-4-carboxylic acids (31)-(35) can be effected under basic conditions.Gas-phase pyrolysis of the N-aryl derivatives (13)-(16) at 550 deg C and 10E-2 Torr gives N-arylpyridazin-3-ones (38)-(41) while the N-t-butyl derivatives (18) and (19) at 750 deg C and 10E-2 Torr give N-unsubstituted pyridazin-3-ones (44) and (45) by additional loss of 2-methylpropene. 2-t-Butylpyridazin-3-ones (42) and (43) can be isolated from the same precursors under milder conditions (500 deg C and 10E-2 Torr).Pyrolysis of the N,N-dimethyl derivative (17) gave only polymeric material.
- McNab, Hamish,Stobie, Ian
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p. 1845 - 1854
(2007/10/02)
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- Lactone Chemistry. Synthesis of β-Substituted, γ-Functionalized Butanolides and Butenolides and Succinaldehydic Acids from Glyoxylic Acid
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The Mannich-type aminoalkylation reaction of enolizable aldehydes with morpholine and glyoxylic acid instead of formaldehyde was investigated: in basic and neutral media were obtained α,γ-dimorpholinobutanolides 2 and α-morpholino-γ-hydroxybutanolides 1, respectively.In acidic medium the spontaneous elimination of the α-morpholino group afforded the γ-hydroxybutenolide 8.The reaction pathways were suggested from the isolation and characterization of some intermediates of the Mannich reaction.These lactone structures constitute versatile synthetic intermediates for the preparation of β-substituted succinaldehydic acids 15 and 5-substituted 3-(2H)-pyridazinones 13 and 14.
- Bourguignon, J. J.,Wermuth, C. G.
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p. 4889 - 4894
(2007/10/02)
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