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.
Preparation of 3-(2-Chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one, a Key Intermediate for the Synthesis of Paliperidone
A PROCESS FOR THE PREPARATION OF PALIPERIDONE INTERMEDIATES
The present invention relates to a process for the preparation of 3-(2-chloroethyl)-6, 7, 8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]-pyrimidin-4-one; and its use in the synthesis of paliperidone.
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(2009/12/05)
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