- 6-Cycloalkyl-pyrazolopyrimidinones for the Treatment of CNS Disorders
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The invention relates to novel 6-Cycloalkyl-pyrazolopyrimidinones according to formula (I). wherein R1 is a 5 or 6 membered aromatic heteroaryl-group, R2 is an optional substituent, D is optionally substituted cyclopentyl, cyclohexyl
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Page/Page column 34
(2012/08/27)
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- 6 - CYCLOBUTYL - 1, 5 - DIHYDRO - PYRAZOLO [3, 4-D] PYRIMIDIN- 4 - ONE DERIVATIVES THEIR USE AS PDE9A INHIBITORS
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The invention relates to novel pyrazolopyrimidinones according to formula (I), wherein R1 is a pyridyl or pyrimidinyl group and D is optionally substituted cyclopentyl, cyclohexyl, tetrahydrofuranyl, tetrahydropyranyl or 2-, 3-or 4-pyridyl. The
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Page/Page column 43
(2012/09/10)
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- Concise synthesis of 1H-pyrazin-2-ones and 2-aminopyrazines
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Convenient syntheses of 1H-pyrazin-2-ones and 2-aminopyrazines are described. By coupling Boc-protected amino acids with α-amino ketones or with amino alcohols and subsequent oxidation, 1H-pyrazin-2-ones were obtained. Transformation into the corresponding pyrazine triflates and substitution with primary or secondary amines led to 2-aminopyrazines. Since these syntheses take advantage of the use of readily available starting materials (e.g., amino acids, aminoalcohols and amines) a variety of the entitled structures can be obtained in few, high yielding steps.
- Adam, Isabelle,Orain, David,Meier, Peter
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p. 2031 - 2033
(2007/10/03)
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- Pyrrolomorphinans as δ opioid receptor antagonists. The role of steric hindrance in conferring selectivity
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A series of 2',3'-disubstituted pyrrolomorphinans (5a-i) were synthesized to determine the role of steric hindrance at μ and γ receptors in promoting δ opioid receptor antagonist selectivity. In smooth muscle preparations, five members of the series (5a-c,e,f) possessed K(e) values in the range 2-15 nM and were 6 selective. Since the unsubstituted analogue 4 possessed δ antagonist potency of similar magnitude, but was not δ selective, it is suggested that the 2',3'substitution confers δ selectivity by hindering the interaction of the pharmacophore at μ and γ receptors, while not affecting δ receptors.
- Farouz-Grant,Portoghese
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p. 1977 - 1981
(2007/10/03)
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- Electrolytic Oxidation of Ketones in Ammoniacal Methanol in the Presence of Catalytic Amounts of KI
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The indirect electrooxidation of ketones in ammoniacal methanol using iodide ion as a mediator afforded 2,2-dialkyl-2,5-dihydro-1H-imidazoles 3 via an oxidative cyclocoupling of ketimine intermediates formed from ketones and ammonia.The treatment of 3 with dilute HCl gave α-amino ketone hydrochlorides 4 and the parent ketones in good yields.A similar electrooxidation of 3 resulted in the formation of the corresponding 2H-imidazoles 6, which were hydrolyzed to α-diketones and the parent ketones.The same products 6 could also conveniently be obtained by chemical oxidation of 3 with aqueous NaOCl.
- Chiba, Toshiro,Sakagami, Hirotoshi,Murata, Miki,Okimoto, Mitsuhiro
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p. 6764 - 6770
(2007/10/03)
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- Ether isonitriles and radiolabeled complexes thereof
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Ether-substituted isonitriles, Tc99m complexes thereof, and processes for myocardial tissue radioimaging using the Tc99m complexes.
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- SYNTHESIS OF α-AMINO KETONE HYDROCHLORIDES VIA CHEMOSELECTIVE HYDROGENATION OF α-NITRO KETONES
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Chemoselective hydrogenation of various α-nitro ketones was accomplished with 5percent Pt sulfide on carbon as a catalyst to afford α-amino ketone hydrochlorides in good yields.
- Tamura, Rui,Oda, Daihei,Kurokawa, Hiroshi
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p. 5759 - 5762
(2007/10/02)
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