- Synthesis process of paliperidone palmitate
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Belonging to the technical field of pharmaceutical compositions, the invention relates to a synthesis process of paliperidone palmitate. Through synthesis of P (paliperidone), refinement of P synthesis of PP (paliperidone palmitate) and refinement of PP, the paliperidone palmitate can be prepared. According to the invention, the process is controllable, the cost is low, the impurities are controllable, the refining process is simple and convenient, the product purity is high, and the yield is high.
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Paragraph 0036; 0046-0051; 0061-0066; 0076-0080
(2019/10/04)
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- PREPARATION OF 3-[2-[4-((6-FLUORO-1, 2-BENZISOXAZOL-3-YL)-L-PIPERIDINYL)-6, 7, 8, 9-TETRAHYDRO-9-HYDROXY-2-METHYL-4H-PYRIDO[ 1, 2-A]-PYRIMIDIN-4-ONE (PALIPERIDONE) AND PALIPERIDONE PALMITATE.
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An improved process for the synthesis of 3-[2-[4-((6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]-pyrimidin-4-one (Paliperidone) and Paliperidone Palmitate through a novel intermediate (2-Chloroethyl)-6,7,8,9-tetrahydro-2-methyl-9-hydroxy-4H-pyrido [1,2-a]pyrimidine-4-one Palmitate ester.
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Paragraph 0038; 0039
(2014/03/25)
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- PREPARATION OF 3-[2-[4-((6-FLUORO-1, 2-BENZISOXAZOL-3-YL)-L-PIPERIDINYL)-6, 7, 8, 9-TETRAHYDRO-9-HYDROXY-2-METHYL-4H-PYRIDO[ 1, 2-A]-PYRIMIDIN-4-ONE (PALIPERIDONE) AND PALIPERIDONE PALMITATE.
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Provided is a process for the synthesis of 3-[2-[4-((6-fluoro-1,2-benzisoxazol-3-y l)-1-piperidinyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]-pyrimidin -4-one (Paliperidone) and Paliperidone Palmitate through a novel intermediate 3-(2-chloroethyl)-6,7,8,9-tetrahydro-2-methyl-9-hydroxy-4H-pyrido[1,2-a]pyrimidin -4-one palmitate ester. A process for preparing a compound of formula VIII through a compound of formula VII is also provide.
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Page/Page column 11-12
(2013/02/28)
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- PROCESSES FOR THE PREPARATION AND PURIFICATION OF PALIPERIDONE PALMITATE
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The present invention encompasses processes for the preparation and purification of paliperidone palmitate.
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Page/Page column 9; 26
(2009/09/04)
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