- Synthesis of α-aminonitriles under mild catalytic, metal-free conditions
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α-Aminonitriles have been synthesized by a Strecker synthesis from aldehydes and ketones under mild catalytic, metal-free conditions. Aromatic aldehydes (1 equiv) were reacted with aromatic and 1 or 2 aliphatic amines (1 equiv) in EtOH containing 3 mol %
- Nammalwar, Baskar,Fortenberry, Chelsea,Bunce, Richard A.
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supporting information
p. 379 - 381
(2014/01/06)
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- 1,3-dihydro-2H-imidazo-[4,5-beta]quinolin-2-one derivatives and intermediates
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The present invention relates to novel 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives of formula (I) wherein R is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl optionally substituted with from 1 to 3 substituents each independently selected from ha
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- 1,3-Dihydro-2H-imidazo[4,5-B]quinolin-2-one derivatives
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Novel 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives of formula STR1 wherein R is hydrogen, C1-6 alkyl, C3-6 cycloalkyl, phenyl optionally substituted with from 1 to 3 substituents each independently selected from halo, hydr
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- Intermediates for the preparation of 1,3,dihydro-2H-imidazo[4,5-B]quinolin-2-one derivatives
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The present invention relates to compounds of the formula STR1 wherein R represents hydrogen; C1-6 alkyl; C3-6 cycloalkyl; phenyl optionally substituted with from 1 to 3 substituents each independently selected from halo, hydroxy, C1-6 alkyloxy, C5-6 cycloalkyloxy, C1-6 alkyl or trifluoromethyl; pyridinyl; or thienyl optionally substituted with halo or C1-6 alkyl; and =C=X is a radical of the formula: the addition salts thereof and stereochemically isomeric forms thereof, said compounds being useful as intermediate to potent inhibitors of both phosphodiesterase III and IV, which are useful in the treatment of warm-blooded animals suffering from allergic disorders, atopic diseases and related afflications.
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- Glycosylated Derivatives of Benzophenone, Benzhydrol, and Benzhydril as Potential Venous Antithrombotic Agents
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A series of glycosylated derivatives of benzophenone, benzhydrol, and benzhydril has been synthesized and evaluated for potential activity as venous antithrombotic agents.Studies on structure-activity relationships revealed that compounds having an electr
- Bellamy, Francois,Horton, Derek,Millet, Jean,Picart, Francois,Samreth, Soth,Chazan, Jean Bernard
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p. 898 - 903
(2007/10/02)
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- Steric Inhibition of Synergistic Radical Stabilizing Effects
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Equilibrium acidities in Me2SO for 14 α-N-morpholinyl-, 6 α-N-piperidinyl-, and 7 α-cyclohexylarylacetonitriles and the oxidation potentials of their conjugate bases have been determined.The increased pKHA values by about 2 units observed in these systems, relative to the corresponding arylacetonitriles, is ascribed to the presence of increased steric constraints in the anions.Hammett plots revealed larger ρ values than for arylacetonitriles (6-7 versus 5.5), pointing to an increased negative charge density on the benzylic carbon atoms in the anions.A plot of anion oxidation potentials, Eox(A-), versus pKHA for the α-N-morpholinylarylacetonitriles was linear with a slope near unity, showing that remote substituents for the most part have very little effect on radical stabilities.A 5 and 6 kcal/mol lowering of the BDE of the acidic C-H bond caused by replacing the cyclohexyl group in α-cyclohexylphenylacetonitrile by α-N-morpholinyl or N-piperidinyl groups, respectively, is attributed to the strong donor properties of these amino functions.The effects are only about one-third as large, however, as similar effects in R2NCH2COPh, where the steric effect of Ph is absent and a synergistic effect is believed to be operative.
- Bordwell, F. G.,Bausch, Mark J.,Cheng, Jin-Pei,Cripe, Thomas H.,Lynch, Tsuei-Yun,Mueller, Mark E.
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