- Preparation method for paliperidone palmitate
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The invention discloses a preparation method for paliperidone palmitate. The preparation method comprises the following steps: step 1, synthesis of 3-(2-hydroxyethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyltetrahydro-pyridino[1,2-alpha]pyrimidin-4-one; step 2, synthesis of 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyltetrahydro-pyridino[1,2-alpha]pyrimidin-4-one; step 3, synthesis of paliperidone; and step 4, synthesis of paliperidone palmitate. Compared with the prior art, the preparation method provided by the invention has the advantages of short reaction time, low cost, controllability of impurities, easiness in purification, high product purity and high yield.
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- Synthesis and absolute configuration assignment of 9-hydroxyrisperidone enantiomers
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The enantiomers of 9-hydroxyrisperidone, the major metabolite of risperidone and the active component of the antipsychotic drug Invega , were synthesized by efficient methods. Their optical rotation and enantiomeric purity were characterized for the first time. The absolute configurations were assigned by comparing 1H NMR chemical shifts of Mosher esters of a key stereoisomeric intermediate. Thus, the stereoisomeric center of (+)-9-hydroxyrisperidone has been assigned as the S configuration, and its enantiomer has the configuration R.
- Xu, Weichu,Wright, George E.,Yanachkova, Milka,Yanachkov, Ivan B.
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p. 470 - 473
(2014/05/20)
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- NOVEL AND IMPROVED PROCESSES FOR THE PREPARATION OF PALIPERIDONE
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The present invention relates to a novel process for the preparation of paliperidone and its intermediates and also relates to an improved process for the preparation of paliperidone compound of formula (I).
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- Prolonged release multiparticulate pharmaceutical composition comprising paliperidone
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The present application pertains to pharmaceutical compositions comprising paliperidone or a pharmaceutically acceptable salt thereof as the active substance, wherein the pharmaceutical composition is in the form of pellets comprising a core particle, optionally one or more intermediate coatings, at least one prolonged release coating and optionally one or more outer coatings, in this order, wherein the active substance is present in the core particle, and wherein the pellets have a maximum diameter of 2 mm or less and exhibit favourable release characteristics.
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- PREPARATION OF PALIPERIDONE
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Processes for preparing paliperidone.
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