- Extension of the Eschweiler-Clarke procedure to the N-alkylation of amides
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The selective N-alkylation of amides (cyclic or acyclic) under hydrogen is reported using aldehydes or ketones as alkylating agents and Pd/C/Na2SO4 as catalyst. Good isolated yields are obtained (81% to 98%).
- Fache, Fabienne,Jacquot, Laurent,Lemaire, Marc
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Read Online
- Tick repellents. II: N-substituted azacyclopentanones and azacyclopentenones
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Several N-substituted azacyclopentanones were synthesized and evaluated as repellents for the brown dog tick Rhipicephalus sanguineus. Several of these compounds were more effective in our test system than were the standard repellents, N,N-dimethyl-m-toluamide and butopyranoxyl.
- Skinner,Rosentreter,Elward
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Read Online
- Process for the preparation of N-substituted lactams
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The invention relates to a process for the preparation of N-substituted lactams by reaction of a lactam, which is unsubstituted on the nitrogen, with an organic halide in the presence of at least one solid-liquid phase transfer catalyst, such as a quaternary ammonium salt, and of at least one solid inorganic base, such as an alkali metal hydroxide, and in the absence of solvent. By this process, N-substituted lactams are obtained with good yields and high purity. The absence of solvent makes possible a considerable gain in productivity and an improvement in safety and in regard for the environment.
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- Reductive O- and N-alkylations. Alternative catalytic methods to nucleophilic substitution
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Different amides have been selectively mono-N-alkylated using catalytic heterogeneous palladium and carbonyl compounds as alkylating agents. The same salt free method has been applied to the synthesis of ethers from alcohols. Reaction parameters have been studied in detail and a mechanism is proposed.
- Fache, Fabienne,Bethmont, Valerie,Jacquot, Laurent,Lemaire, Marc
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p. 231 - 238
(2007/10/03)
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- N-allyl-lactams as crystallization inhibitors
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Crystallization of active material in spraying of an aqueous solution of certain specified fungicides is retarded by incorporation therein of an N-alkyl-lactam of the formula STR1 in which R represents alkyl having 6 to 18 carbon atoms and n represents the numbers 3, 4 or 5.
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- N-alkyl-lactams as crystallization inhibitors
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In the spraying of an aqueous liquor comprising at least one of 1-(4-chlorophenyl)-4,4-dimethyl-3-(1,2,4-triazol-1-yl-methyl)-pentan-3-ol and 1-(4-chlorophenoxy)-3,3-dimethyl-1-(1,2,4-triazol-1-yl)-butan-2-ol, the improvement which comprises including in the liquor an N-alkyl-lactam of the formula STR1 in which R represents alkyl having 8 to 18 carbon atoms and n represents the numbers 3, 4 or 5,
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- Solid formulations
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New solid formulations of A) at least one agrochemical active compound, B) at least one additive from the groups mentioned in the description, C) at least one dispersant, D) at least one carrier and E) if appropriate, further active compounds and/or additives, a process for preparing the solid formulations and their use for treating plants. A new device for preparing new granules.
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- Composition comprising an oxygenated cholesterol and use thereof for topical treatment of diseases
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The invention is directed to a pharmaceutical composition comprising an oxygenated cholesterol and a penetration-enhancing agent which is useful for topical application to the skin of a patient suffering from a proliferative skin disease characterized by geminative cells having a rapid rate of replication, e.g. psoriasis. The composition comprises an effective amount for the inhibition of germinative cell mitosis of an oxygenated cholesterol, e.g. 26-hydroxycholesterol, or a pharmaceutically effective derivative thereof e.g. an ester or ether. The invention is further directed to a method of treating a patient suffering from said skin disease comprising applying to the effected skin said therapeutic composition. The invention is also directed to the topical application of these compositions to the skin to decrease inflammation.
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- Physiological vehicle compositions containing higher alkyl substituted azacyclopentan-2-ones
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There is disclosed an improved method for topically administering a physiologically active agent to a human or animal by dissolving an effective amount of the agent in a carrier containing suitable amounts of 1-alkyl substituted-azacyclopentan-2-one, as defined herein, and contacting the skin or other membranes of the human or animal with the resulting composition, whereby penetration of the skin or membranes is enhanced.
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