SPIROPIPERIDINE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
The present invention is directed to spiropiperidine compounds of formula (I) and tautomers thereof, which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as
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Page/Page column 33-34
(2010/11/25)
JOINT EFFECT OF THE TEMPERATURE AND THE POLARITY OF THE MEDIUM ON THE RATE OF THE REACTION OF 3,5-DINITROBENZOYL CHLORIDE WITH 3-FLUOROANILINE. ISOPARAMETRIC POINT IN THE VARIABLE PARAMETERS
The rate of acylation of 3-fluoroaniline by 3,5-dinitrobenzoyl chloride at 283, 290, 298, and 313 K was measured in nonspecifically solvating media with various polarities (chlorobenzene and its binary mixtures with nitrobenzene and cyclohexane).The kinetic data were treated by means of the Kirkwood and Arrhenius equations with one variable parameter and by crossed correlation with two varible parameters.Bends were found on the curves for the reaction rate and also for the activation parameters against the polarity of the medium.It was found that the mutual effect of the variable factors on the process rate is nonadditive in nature.It was shown that the polarity of the transition states decreases substantially with substitution of the nitrobenzene in the mixtures by cyclohexane.The existence of isoparametric points with respect to temperature and to the medium in the reactions taking place in low-polarity solvents was demonstrated experimentally.The results from the correlation analysis are consistent with the participation of cyclic transition states in acyclation in low-polarity media.
Shpan'ko, I. V.,Goncharov, A. N.
p. 2287 - 2291
(2007/10/02)
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