Oxidative degradation of paliperidone using potassium permangnate in acid medium
Oxidative degradation reactions of paliperidone are studied using potassium permanganate in acidic medium spectrophotometrically. Complete reaction was carried out in pseudo first order condition. The reaction orders were calculated with respect to the paliperidone and acid, the obtained values indicate that these reactant have less than first order dependency on the reaction rate. Oxidation products were identified using LC-MS technique and their m/z values were found to be 207, 221 and 443. Kinetics and the mechanism of the reactions were derived from the results identified. The reactions were studied at four different temperatures with different paliperidone and acid concentrations. The activation and thermodynamic parameters were calculated by graphical method.
4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable stearoyl-CoA desaturase-1 (SCD1) inhibitors: Part 2. Pyridazine-based analogs
Design, synthesis, and biological evaluation of pyridazine-based, 4-bicyclic heteroaryl-piperidine derivatives as potent stearoyl-CoA desaturase-1 (SCD1) inhibitors are described. In a chronic study of selected analog (3e) in Zucker fa/fa (ZF) rat, dose-dependent decrease of body weight gain and plasma fatty acid desaturation index (DI) in both C16 and C18 are also demonstrated. The results indicate that the plasma fatty acid DI may serve as an indicator for direct target engagement and biomarker for SCD1 inhibition.
Yang, Shyh-Ming,Tang, Yuting,Rano, Thomas,Lu, Huajun,Kuo, Gee-Hong,Gaul, Michael D.,Li, Yaxin,Ho, George,Lang, Wensheng,Conway, James G.,Liang, Yin,Lenhard, James M.,Demarest, Keith T.,Murray, William V.
supporting information
p. 1437 - 1441
(2014/03/21)
Process for making risperidone and intermediates therefor
The formation of risperidone is enhanced by the use of enriched Z-isomer oxime intermediate(s) of formula (3) or (7). The oxime(s) can be isomerically enriched by a variety of techniques including the use of the novel acetic acid salt thereof, which affords, inter alia, resolution of the isomers and/or by heat conversion.
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Page/Page column 5
(2008/06/13)
Inhibitors of serotonin reuptake
This invention provides compounds and a method for the inhibition of serotonin reuptake in mammals.
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(2008/06/13)
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