- METHODS AND COMPOSITIONS FOR TREATMENT OF CANCER
-
In an aspect, the disclosure pertains to inhibitors of ANGPTL4; synthesis methods for making disclosed compounds; pharmaceutical compositions comprising disclosed compounds; methods of treating disorders of uncontrolled cellular proliferation, e.g., a cancer; and methods of treating a disease associated with an ANGPTL4 dysfunction using disclosed compounds and pharmaceutical compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
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Paragraph 0135; 0137
(2021/07/30)
-
- Synthesis process of paliperidone palmitate
-
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 0036-0045; 0051-0060; 0066-0075
(2019/10/04)
-
- Paliperidone intermediate and method for producing paliperidone using the same
-
Disclosed are novel intermediates of paliperidone which are used as a therapeutic agent for schizophrenia, and to a method for producing paliperidone using the same. The intermediates are a compound represented by chemical formula 3 and a compound represented by chemical formula 5. The method for producing paliperidone comprises a step of conducting a reaction of a compound represented by chemical formula 5 and an acid compound. In the chemical formulas 3 and 5, R is a silyl group, a hydrocarbon group having 1-20 carbon atoms, a protecting group represented by -R_1OR_2 or -R_1SR_2, or a protecting group represented by -C(=O)R_2. In particular, R_1 is a methylene group or a carbonyl group, and R_2 is a substituted or unsubstituted alkyl group, an aryl group, or an alkylaryl group, wherein R_1 and R_2 can bond to each other to form a ring.COPYRIGHT KIPO 2018
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- New synthesis method of paliperidone
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The invention relates to a new synthesis method of paliperidone. 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride and 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one which are used as starting materials are reacted in the presence of a reducing reagent and an acid binding agent to obtain the paliperidone. The reducing agent is added in the reaction, so side reactions are reduced, the content of every impurity in the obtained finished product is significantly reduced, especially the content of the key impurity A is significantly reduced, the product has a high purity, and the method is simple to operate, and is suitable for industrial production.
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Paragraph 0025; 0026; 0028; 0030; 0032; 0034; 0036; 0038
(2018/07/30)
-
- Preparation method of palipefidone
-
The invention provides a preparation method of palipefidone. The preparation method comprises the following steps: dissolving a palipefidone crude product into a heated alcohol solution; adding active carbon under a heating condition; keeping heat and stirring; filtering when the solution is hot to obtain a filtrate; at a temperature of 45 DEG C to 60 DEG C, adding a reducing agent into the filtrate, and keeping the heat and stirring for 30 to 60 minutes; after stirring, controlling to cool for 8 DEG C to 15 DEG C every hour; slowly cooling and crystallizing; after crystallizing, filtering to obtain a solid and a refined mother solution respectively; performing water washing, alcohol washing and vacuum drying on the obtained solid to obtain palipefidone crystallized powder; decompressing and concentrating the refined mother solution and recycling palipefidone secondary precipitate. The preparation method of the palipefidone is simple in process and convenient to operate, does not need special equipment and is suitable for industrial production; a toxin-free or low-toxin solvent is adopted, so that environmental pollution is lowered; the prepared product has high purity, and the content of 9-keto impurities is reduced to be 0.05 percent, even lower.
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Paragraph 0072; 0073; 0074; 0075; 0076
(2016/10/10)
-
- A is suitable for industrial production of high-purity 9-hydroxy-risperidone
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The invention discloses a method suitable for industrial production of high-purity 9-hydroxy-risperidone. According to the method, the 9-hydroxy-risperidone is prepared by carrying out condensation on 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole and 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]-pyrimidin-4-one in a polar solvent system; by optimizing post-treatment operation and improving a refining method, the high-yield and high-purity 9-hydroxy-risperidone can be prepared by utilizing the steps of sedimentation, salifying, alkali regulation, crystallization and the like; the post-treatment and the refining method disclosed by the invention has the advantages of simplicity and convenience in operation, low production cost and high product purity and are suitable for use in the industrial production.
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Paragraph 0035; 0036; 0037; 0038; 0039
(2017/03/23)
-
- 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.
-
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 0040; 0041
(2014/03/25)
-
- Green Synthesis of 3-(2-(4-(6-Fluorobenzo[d]isoxazol-3-yl)piperidin-yl) ethyl-6,7,8,9-tetrahydro-9-hydroxy-2-methylpyridol[1,2-a]pyrimidin-4-one
-
Paliperidone has been synthesized in high yields by condensation of 3-(2-chloroethyl)-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyridol[ 1,2a]pyrimidin-4-one (1) and (2,4-difluoro-phenyl)-piperidin-4-yl-methanone oxime (2) using K2CO3 as a base, refluxing in acetonitrile for 16 h. The novel intermediate (3) underwent internal cyclization in PEG-600 as solvent yielded paliperidone (4). Paliperidone (4) from novel intermediate (3) has also been prepared under microwave condition using PEG-600 and also in presence of a base KOH in toluene at 70 °C for 3 h in higher yields.
- Reddy, D. Vivekananda,Sreelatha,Dubey,Devi, Rama
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p. 3450 - 3452
(2014/08/05)
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- PROCESS FOR THE PREPARATION OF PALIPERIDONE
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The present invention provides a process for the preparation of paliperidone or a pharmaceutically acceptable salt thereof, wherein the process comprises condensing a compound of formula (II) with a compound of formula (III) or a salt thereof, in a suitable solvent and a base, in the presence of a catalyst and an inhibiting agent, wherein the inhibiting agent is added to the reaction system before the compound of formula (II) and compound of formula (III) have reacted or as the reaction of the compound of formula (II) and compound of formula (III) is initiated, and optionally converting the paliperidone to a salt thereof, wherein X is a suitable leaving group. The present invention also provides substantially pure paliperidone or a salt thereof, paliperidone or a salt thereof as prepared by the process and uses of the paliperidone or salt thereof.
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Paragraph 0097; 0098; 0099
(2014/07/23)
-
- Processes for the preparation of paliperidone
-
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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- 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.
-
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 12
(2013/02/28)
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- AN IMPROVED PROCESS FOR THE PREPARATION OF PALIPERIDONE
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The present invention relates to a process for preparation and purification of 3-[2-[4-(6- fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H- pyrido[1,2-a]pyrimidin-4-one, also known as paliperidone or 9-hydroxy risperidone.
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- Novel Process for the Preparation of Paliperidone
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The present invention relates to a novel process for the preparation of paliperidone by hydrolysis of 9-O-acylated paliperidone. In a preferred embodiment of the present invention, Paliperidone Form (II) of purity of about 98% or more was obtained by basic hydrolysis of 9-O-Acetyl Paliperidone.
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Page/Page column 8
(2012/10/18)
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- PROCESS FOR PREPARATION OF PALIPERIDONE
-
The present invention relates to an improved process for the preparation of pure Paliperidone of Formula I.
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- SOLID STATE FORMS OF PALIPERIDONE SALTS AND PROCESS FOR THE PREPARATION THEREOF
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Provided herein are solid state forms of paliperidone salts, processes for preparation, pharmaceutical compositions, and method of treating thereof. Paliperidone is represented by the following structural formula (I): More particularly, provided are solid state forms of paliperidone acid addition salts, wherein the acid counter ion is provided by an acid selected from the group consisting of L-(+)-tartaric acid, p-toluenesulfonic acid, maleic acid, oxalic acid, fumaric acid, acetic acid and malic acid. Provided also herein is a process for preparing substantially pure paliperidone free base using the solid state forms of paliperidone salts.
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Page/Page column 10
(2012/05/04)
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- AN IMPROVED PROCESS FOR THE PREPARATION OF HIGHLY PURE PALIPERIDONE
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An improved process for the preparation of pure paliperidone which is substantially free from impurity namely, keto paliperidone. 3-(2-chloroethyl)-9-hydroxy-2-methyl-6,7,8,9-tetrahydro- 4H-pyrido[1,2-a]-pyrimidin-4-one is condensed with 6-fluoro-3-piperidin-4-yl-1,2- benzisoxazole hydrochloride or a salt thereof in the presence of solvent, base and a catalyst to obtain crude paliperidone. The crude paliperidone is purified by treating it with solvent in presence of base at reflux temperature to obtain clear solution which is cooled to crystallizing out pure paliperidone.
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Page/Page column 14
(2012/04/04)
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- PROCESS FOR THE PREPARATION OF PURE PALIPERIDONE
-
The present invention relates to an improved process for the preparation of pure Paliperidone of formula (I). The present invention more specifically provides an improved process for the preparation of pure Paliperidone which may contain impurities in the acceptable level of pharmacopoeia requirement specifically 3-{2-[4-(5-Fluoro-benzo[d]isoxazol-3-yl]-piperidin-1-yl]-ethyl}-2-methyl-7,8-dihydro-6H-pyrido[1,2-a]pyrimidine-4,9-dione of Formula (IV).
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Page/Page column 2-3
(2012/07/13)
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- PROCESS FOR THE PREPARATION OF PALIPERIDONE
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The present invention provides a process for the preparation of paliperidone or a pharmaceutically acceptable salt thereof, wherein the process comprises condensing a compound of formula (II) with a compound of formula (III) or a salt thereof, in a suitable solvent and a base, in the presence of a catalyst and an inhibiting agent, wherein the inhibiting agent is added to the reaction system before the compound of formula (II) and compound of formula (III) have reacted or as the reaction of the compound of formula (II) and compound of formula (III) is initiated, and optionally converting the paliperidone to a salt thereof, wherein X is a suitable leaving group. The present invention also provides substantially pure paliperidone or a salt thereof, paliperidone or a salt thereof as prepared by the process and uses of the paliperidone or salt thereof.
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Page/Page column 19
(2013/02/28)
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- Selective chemical oxidation of risperidone: A straightforward and cost-effective synthesis of paliperidone
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A very short and cost-effective synthesis of the commercial drug paliperidone has been achieved starting from its parent compound risperidone, through a thoroughly optimized oxidation with air under basic conditions. A very short and cost-effective synthesis of the commercial drug paliperidone (1) has been achieved starting from its parent compound risperidone, through a thoroughly optimized oxidation with air under basic conditions. Copyright
- Riva, Renata,Banfi, Luca,Castaldi, Graziano,Ghislieri, Diego,Malpezzi, Luciana,Musumeci, Francesca,Tufaro, Roberto,Rasparini, Marcello
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experimental part
p. 2319 - 2325
(2011/06/22)
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- A NOVEL PROCESS FOR THE PREPARATION OF PALIPERIDONE
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The present invention relates to a novel process for the preparation of paliperidone by hydrolysis of 9-O-acylated paliperidone. In a preferred embodiment of the present invention, Paliperidone Form (II) of purity of about 98% or more was obtained by basic hydrolysis of 9-O-Acetyl Paliperidone.
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Page/Page column 14
(2011/07/07)
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- PROCESS FOR PREPARING PALIPERIDONE AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
-
The present invention discloses the process for the preparation of paliperidone and its pharmaceutically acceptable salts comprising (a) condensing 2-amino-3-hydroxy- pyridine with 2-acetylbutyro lactone in the presence of an acid catalyst to isolate 9- hydroxy-3-(2-hydroxyethyl)-2-rnethyl-4H-pyrido[l, 2-a] pyrimidin-4-one; treating 9- hydroxy-3-(2-hydroxyethyl)-2-methyl-4H-pyrido[l, 2-a] pyrimidin-4-one with a chlorinating agent; hydrogenating the product in the presence of one or more lewis acids to obtain 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[l,2-a]- pyrimidin-4-one; and condensing3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2- methyl-4H-pyrrido[l,2-a]-pyrimidin-4-one. The present invention also discloses processes for the preparation of intermediates useful in the preparation of paliperidone and its pharmaceutically acceptable salts.
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- A PROCESS FOR THE PURIFICATION OF PALIPERIDONE
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The process comprises submitting crude Paliperidone to an esterification reaction in the presence of a basic agent to yield a compound of formula (III), wherein n is 1-8. This process gives the Paliperidone with high purity after hydrolysis.
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Page/Page column 18
(2011/06/25)
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- A process for the purification of paliperidone
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The process comprises submitting crude Paliperidone to an esterification reaction in the presence of a basic agent to yield a compound of formula (III), wherein n is 1-8. This process gives Paliperidone with high purity after hydrolysis.
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Page/Page column 9
(2011/08/03)
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- PALIPERIDONE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF SUBSTANTIALLY FREE OF IMPURITIES
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Provided herein are impurities of paliperidone, 3-[2-[4-[l-(4-fruoro-2-hydroxyphenyl) methanoyl]piperidinyl-l-yl]ethyl]-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[l,2-a]pyrimidin-4- one (methanoyl impurity), 3-[2-[4-(6-fluoro-l,2-benzisoxazol-3-yl)-l-piperidinyl]ethyl]-2- methyl-4H-pyrido[l,2-a]pyrimidin-4-one (dehydroxy impurity) and 3-[2-[4-(6-fluoro-l,2- benzisoxazol-3-yl)-l-piperidinyl]ethyl]-2-methyl-7,8-dihydro-6H-pyrido[l,2-a]pyrimidin- 4,9-dione (9-keto impurity), and processes for preparing and isolating thereof. Provided further herein is a highly pure paliperidone or a pharmaceutically acceptable salt thereof substantially free of methanoyl, dehydroxy and 9-keto impurities, process for the preparation thereof, and pharmaceutical compositions comprising highly pure paliperidone or a pharmaceutically acceptable salt thereof substantially free of methanoyl, dehydroxy and 9- keto impurities. Provided also herein are improved and efficient processes for preparing paliperidone intermediates.
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Page/Page column 45-46
(2011/04/18)
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- AN IMPROVED PROCESS FOR THE PREPARATION OF PURE PALIPERIDONE
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The present invention relates to an improved process for the preparation of pure Paliperidone of formula (I). The present invention more specifically provides an improved process for the preparation of pure Paliperidone which may contain impurities in the acceptable level of pharmacopoeia requirement specifically 3-{2-[4-(5-Fluoro-benzo[d]isoxazol-3-yl]-piperidin-1-yl]-ethyl}-2- methyl-7,8-dihydro-6H-pyrido[1,2-a]pyrimidine-4,9-dione of Formula (IV).
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Page/Page column 9
(2011/02/24)
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- Process for the synthesis of paliperidone
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The invention describes an improved process for the synthesis and purification of paliperidone.
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Page/Page column 5-6
(2011/02/18)
-
- PROCESS FOR THE SYNTHESIS OF PALIPERIDONE
-
The invention describes an improved process for the synthesis and purification of paliperidone.
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Page/Page column 13
(2011/02/24)
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- One-step process for preparing paliperidone and its oxalate salt
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The present invention relates to a one-step process for the preparation of the antipsychotic agent Paliperidone by oxidation of Risperidone, and to Paliperidone oxalate or a hydrate, solvate or polymorph thereof.
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Page/Page column 6
(2010/07/06)
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- PROCESS OF SYNTHESIS OF PALIPERIDONE
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The invention relates to an improved process for preparation of 3-(2-chloroethyl)-9-hydroxy-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one, an intermediate used in the synthesis of paliperidone and process for converting the same to Paliperidone.
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Page/Page column 7
(2010/06/20)
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- SYNTHESIS OF PALIPERIDONE
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A compound of formula (6) or an acid addition salt thereof in which G is (i) a leaving group A selected from a halo group and a sulfonyloxy group, or (ii) a group of the formula (20) is useful in processes of making paliperidone and related compounds.
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Page/Page column 11-12
(2010/02/17)
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- Process for the purification of paliperidone
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Process for the purification of paliperidone by formation of a salt thereof, such as the hydrochloride.
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Page/Page column 6
(2010/11/04)
-
- Purification of paliperidone
-
The present invention relates to a process for the purification of Paliperidone from its impurities by a simple process that can be used at industrial scale, with overall good yields, which reduces the number of crystallisation steps and removes all impurities, yielding Paliperidone of very high purity. Also, the present invention relates to the preparation of pure Paliperidone via Paliperidone salts.
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Page/Page column 7; 8
(2010/07/08)
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- Processes for the Preparation of Paliperidone and Pharmaceutically Acceptable Salts Thereof and Intermediates for Use in the Processes
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The present invention relates to novel compounds of formula (VIII) and (X), processes for their preparation and their use in the preparation of paliperidone or a salt thereof. There is also provided by the present invention novel processes for preparing intermediates for use in the preparation of paliperidone or a salt thereof, and novel processes for preparing paliperidone or a salt thereof.
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Page/Page column 14-15
(2010/12/29)
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- SOLID STATE FORMS OF PALIPERIDONE SALTS AND PROCESS FOR THE PREPARATION THEREOF
-
Provided herein are solid state forms of paliperidone salts, processes for preparation, pharmaceutical compositions, and method of treating thereof. Paliperidone is represented by the following structural formula (I) : More particularly, provided are solid state forms of paliperidone acid addition salts, wherein the acid counter ion is provided by an acid selected from the group consisting of L- (+) -tartaric acid, p- toluenesulfonic acid, maleic acid, oxalic acid, fumaric acid, acetic acid and malic acid. Provided also herein is a process for preparing substantially pure paliperidone free base using the solid state forms of paliperidone salts.
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Page/Page column 25
(2010/12/26)
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- PROCESS FOR THE PURIFICATION OF PALIPERIDONE
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Process for the purification of paliperidone by formation of a salt thereof, such as the hydrochloride.
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Page/Page column 4
(2010/11/03)
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- PREPARATION OF 3-(2-HYDROXY ETHYL)-9-HYDROXY-2-METHYL-4H-PYRIDO-[1,2-A]-PYRIMIDIN-4-ONE OR ITS ACID ADDITION SALT
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The invention relates to an improved process for preparation of 3-(2-hydroxy ethyl)-9- hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one or its acid addition salt and its conversion to paliperidone or its acid addition salt without involving the use of an acid catalyst.
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Page/Page column 8-9
(2010/08/08)
-
- 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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Page/Page column 14; 22
(2010/04/03)
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- NOVEL COMPOUNDS FOR TREATMENT OF PSYCHOTIC DISORDERS, PREPARATION METHODS AND USES THEREOF
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The present invention relates to a compound of formula (I), an optical isomer or a pharmaceutically acceptable salt thereof, its preparation and uses, wherein R is defined as herein. Such compounds can be presented as an optical isomer or a racemic mixture. The compounds can be metabolized in vivo to form a pharmacologically active substance as antagonist of neurotransmitters, and can be used for the treatment of the related mental disorders such as schizophrenia.
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Page/Page column 7
(2010/03/04)
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- PROCESS FOR THE PREPARATION OF PALIPERIDONE
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The present invention belongs to the field of chemical synthesis and relates to an improved process for the preparation of paliperidone and its pharmaceutically acceptable salts as an active ingredient of a medicament for treatment of schizophrenia. It relates also to a process of crystallization of paliperidone and to the dihydrate form of the compound.
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Page/Page column 8
(2010/04/03)
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- NOVEL PROCESS FOR PREPARING PURE 6-FLUORO-3-PIPERIDIN-4-YL-1,2-BENZISOXAZOLE HYDROCHLORIDE AND ITS CONVERSION TO PALIPERIDONE
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The invention relates to novel process for providing substantially pure 6-Fluoro-3- piperidin-4-yl-1,2-benzisoxazole hydrochloride and its conversion to Paliperidone having dimer compound of structural formula-1 A is less than 0.2 % and HPLC purity > 99.7%.
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Page/Page column 6
(2010/08/08)
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- AN IMPROVED PROCESS FOR THE PREPARATION OF PALIPERIDONE
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The invention relates to an improved process for the preparation of Pal?peridone in high yield and purity. The purity of Paliperidone is ~99.7 % by HPLC, wherein total impurity is less than about 0.3 % and each individual impurity is less than about 0.1 %. The invention also relates to provide the alcohol-water co-solvent for the purification of Paliperidone.
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Page/Page column 4
(2010/08/18)
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- PROCESS FOR THE PREPARATION OF PALIPERIDONE AND ITS INTERMEDIATES
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A process for the preparation of a psychotropic agent Paliperidone. Preferably, this invention relates to a method for the purification of Paliperidone by making its acid addition salts.
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Page/Page column 5
(2010/12/29)
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- STABLE POLYMORPHIC FORM OF PALIPERIDONE AND PROCESS FOR ITS PREPARATION
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The present invention relates to stable polymorphic form of paliperidone and process for its preparation. The chemical name of Paliperidone (I) is 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one. Formula (I): Paliperidone is useful as anti-psychotic agent in the treatment of psychotic disorders. Paliperidone is available in market under brand name INVEGA.
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Page/Page column 8
(2009/03/07)
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- PALIPERIDONE DERIVATIVES
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A compound of formula (1) is useful as a pharmaceutical and as an intermediate in making paliperidone. wherein Y is an acid-sensitive group of the formula: in which X represents an oxygen atom, a sulfur atom, or an —NH— group; Z represents a C2-C7 alkylene bridge; and R represents hydrogen or a C1-C4 alkyl group.
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Page/Page column 11-12
(2009/04/24)
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- PREPARATION OF PALIPERIDONE
-
Processes for preparing paliperidone.
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- 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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Page/Page column 15
(2009/12/05)
-
- Highly Pure Paliperidone or a Pharmaceutically Acceptable Salt Thereof Substantially Free of Keto Impurity
-
Provided herein is a highly pure paliperidone or a pharmaceutically acceptable salt thereof substantially free of keto impurity, 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-2-methyl-7,8-dihydro-6H-pyrido[1,2-a]pyrimidin-4,9-dione, a process for the preparation thereof, and pharmaceutical compositions comprising highly pure paliperidone or a pharmaceutically acceptable salt thereof substantially free of keto impurity.
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Page/Page column 8-9
(2009/10/06)
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- PROCESSES FOR PREPARING CRYSTAL FORMS OF 9-HYDROXY-RISPERIDONE (PALIPERIDONE)
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The present invention is related to processes for the preparation of paliperidone crystalline Form II. The invention also provides a paliperidone crystalline Form II containing isopropyl alcohol, and processes for preparing the same.
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Page/Page column 14
(2009/07/03)
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- PROCESS TO PREPARE PALIPERIDONE AND INTERMEDIATES THEREOF
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The present invention relates to an improved process for obtaining Paliperidone, I, comprising alkylating compound VI, or a salt thereof, with compound V, or a salt thereof, using a base selected from triethylamine or diisopropylethylamine and, optionally, a solvent. Moreover, the invention relies on the preparation of intermediates used in such process.
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Page/Page column title page; 3; 5; 14-15; 16
(2009/12/27)
-
- AN IMPROVED, INDUSTRIALLY VIABLE PROCESS FOR THE PREPARATION OF HIGH PURITY PALIPERIDONE
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The present invention relates to an improved and industrially viable process for the preparation of high purity ≥ 99.8% chemical of paliperidone of formula-I (3-[2-[4-(6-fluoro-l,2-benzisoxazol-3-yl)-l-piperidinyl]ethyl]-6,7,8,9-tetra-hydro-9-hydroxy-2- methyl-4H-pyrido[l,2-a]pyrimidin-4-one), involving the novel intermediate, 3-(2- hydroxyethyl)-2-methyl-9-(phenylmethoxy)-4H-Pyrido[l,2-a]pyrimidin-4-one of formula-II. All intermediates encountered in the synthetic pathway of present invention are isolated by simple crystallization techniques in high pure. Paliperidone is useful as anti-psychotic agent in the treatment of psychotic disorders and is marketed under the brand name INVEGA.
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Page/Page column 15-17
(2009/03/07)
-
