- One-Pot Base-Mediated Synthesis of Functionalized Aza-Fused Polycyclic Quinoline Derivatives
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A new one-pot protocol has been developed for the facile and efficient synthesis of aza-fused polycyclic quinolines (e.g., pyrrolo[1,2-a]quinolines) by the base-catalyzed reaction of 2-formylpyrroles and 2-halophenylacetonitriles. This reaction proceeded under transition metal-free conditions and showed high functional group tolerance, with the desired products being formed in good yields.
- Jiang, Zeng-Qiang,Miao, Da-Zhuang,Tong, Yao,Pan, Qiang,Li, Xiao-Tong,Hu, Ren-He,Han, Shi-Qing
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supporting information
p. 1913 - 1921
(2015/06/30)
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- COMPOUNDS FOR THE TREATMENT OF CNS DISORDERS
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The invention relates to novel cycloalkyl- or cycloalkenyl-substituted pyrazolopyrimidinones of formula (I), wherein ā is selected from the group A1 consisting of a C3-C8-cycloalkyl group or a C4-C8-cycloalkenyl group, whereby the members of C3-C8-cycloalkyl group being selected from the group of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptanyl and cyclooctanyl; and the members of the C4-C8-cycloalkenyl group, being selected from cyclobutenyl, cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclooctenyl, cyclopentadienyl, cyclohexadienyl, cycloheptadienyl, cyclooctadienyl, cycloheptatrienyl, cyclooctathenyl, cyclooctatetraenyl. The new compounds shall be used for the manufacture of medicaments, in particular medicaments for improving perception, concentration, learning and/or memory in patients in need thereof. Chemically, the compounds are characterised as pyrazolopyrimidinones with a cycloalkyl-moiety directly bound to the 1 position of the pyrazolopyrimidinone and a second substituent in the 6 position which is bound via an optionally substituted methylene-bridge. Further aspects of the present invention refer to a process for the manufacture of the compounds and their use for producing medicaments.
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Page/Page column 41
(2012/05/20)
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- 1-HETEROCYCLYL-1,5-DIHYDRO-PYRAZOLO[3,4-D] PYRIMIDIN-4-ONE DERIVATIVES AND THEIR USE AS PDE9A MODULATORS
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The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones, Formula (I) with Hc is a mono-, bi- or tricyclic heterocyclyl group, the ring members of which are carbon atoms and at least 1, preferably 1, 2 or 3, heteroatom(s), which are selected from the group of nitrogen, oxygen and sulphur, which is in the form of -S(O)r - with r being 0, 1 or 2, and - said heterocyclyl group is or comprises 1 non-aromatic, saturated, or partly unsaturated monocyclic ring which comprises at least 1 heteroatom as ring member and - said heterocyclyl group is bound to the scaffold by said 1 non- aromatic, saturated, or partly unsaturated monocyclic ring which comprises at least 1 heteroatom as ring member. According to one aspect of the invention the new compounds are for the manufacture of medicaments, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. The new compounds are also for the manufacture of medicaments for the treatment of Alzheimer's disease.
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Page/Page column 163; 167
(2009/10/30)
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- Synthesis of indene derivatives via electrophilic cyclization
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3-Iodo-1H-indene derivatives are synthesized by iodonium-promoted 5-endo-dig carbocyclization of 2-substituted ethynylmalonates. Various 2-substituted ethynylmalonates bearing aryl-, alkyl-and ether-protected propargyl alcohols were successfully converted
- Khan, Zulfiqar Ali,Wirth, Thomas
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supporting information; experimental part
p. 229 - 231
(2009/06/20)
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- Palladium-catalyzed carboxamidation reaction and aldol condensation reaction cascade: A facile approach to ring-fused isoquinolinones
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(Chemical Equation Presented) Palladium-catalyzed carboxamidation reaction and aldol condensation reaction cascade are very useful for the synthesis of various ABC ring substituted fused isoquinolinones.
- Chouhan, Gagan,Alper, Howard
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supporting information; experimental part
p. 4987 - 4990
(2009/05/31)
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- 4,6-O-[1-cyano-2-(2-iodophenyl)ethylidene] acetals. Improved second-generation acetals for the stereoselective formation of β-D-mannopyranosides and regioselective reductive radical fragmentation to β-D-rhamnopyranosides. Scope and limitations
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The [1-cyano-2-(2-iodophenyl)]ethylidene group is introduced as an acetal-protecting group for carbohydrate thioglycoside donors. The group is easily introduced under mild conditions, over short reaction times, and in the presence of a wide variety of oth
- Crich, David,Bowers, Albert A.
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p. 3452 - 3463
(2007/10/03)
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- Synthesis of indenes by the palladium-catalyzed carboannulation of internal alkynes
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(Chemical Equation Presented) A number of highly substituted indenes have been prepared in good yields by treating functionally substituted aryl halides with various internal alkynes in the presence of a palladium catalyst. The reaction is believed to proceed by regioselective arylpalladation of the alkyne and subsequent nucleophilic displacement of the palladium in the resulting vinylpalladium intermediate.
- Zhang, Daohua,Eul, Kgun Yum,Liu, Zhijian,Larock, Richard C.
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p. 4963 - 4966
(2007/10/03)
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