130049-85-3

Basic information

• Product Name: (R)-9-Hydroxy Risperidone
• Synonyms: (R)-9-Hydroxy Risperidone;(9R)-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;(R)-9-Hydroxy Risperidone ((R)-Paliperidone);Paliperidone R-Isomer;(R)-Paliperidone;9-(R)-Paliperidone;3-[2-[4-(6-Fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9(R)-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one
• CAS NO: 130049-85-3
• Molecular Formula: C₂₃H₂₇FN₄O₃
• Molecular Weight: 426.4838832
• Product Categories: Heterocycles;Intermediates & Fine Chemicals;Metabolites & Impurities;Pharmaceuticals;Heterocycles, Metabolites & Impurities, Pharmaceuticals, Intermediates & Fine Chemicals
• Mol File: 130049-85-3.mol
• Article Data: 5

Chemical Properties

• Appearance: /
• CAS DataBase Reference: (R)-9-Hydroxy Risperidone(CAS DataBase Reference)
• NIST Chemistry Reference: (R)-9-Hydroxy Risperidone(130049-85-3)
• EPA Substance Registry System: (R)-9-Hydroxy Risperidone(130049-85-3)

Safety Data

• Hazardous Substances Data: 130049-85-3(Hazardous Substances Data)

Usage

Uses

The R-enantiomer metabolite of Risperidone (R525000), a combined serotonin (5-HT2) and dopamine (D2) receptor antagonist.

Upstream product

• 181525-38-2 9-hydroxy-3-hydroxyethyl-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one 
• 84163-77-9 6-fluoro-3-(4-piperidinyl)benzo[d]isoxazole 
• 1606138-67-3 C₂₁H₂₇ClN₂O₅ 
• 84163-13-3 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride 
• 849727-63-5 (±)-3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one monohydrochloride 
• 147687-17-0 9-(benzyloxy)-3-(2-chloroethyl)-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one 
• 766485-15-8 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidin-1-yl]ethyl]-9-hydroxy-2-methyl-4H-pyrido-[1,2-a]pyrimidin-4-one 
• 1189516-65-1 R₁₂₅₂₃₉ 
• 849727-62-4 3-(2-chloroethyl)-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one monohydrochloride 
• 1138463-56-5 3-(2-chloroethyl)-9-oxo-2-methyl-6,7,8,9-tetrahydro-4H-pyrido-[1,2-a]pyrimidin-4-one 
• 24016-03-3 2-amino-3-benzyloxypyridine 
• 130049-82-0 3-(2-chloroethyl)-9-hydroxy-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one 
• 7087-68-5 N-ethyl-N,N-diisopropylamine 
• 517-23-7 3-acetyl-2-oxo-4,5-dihydrofuran 

Relevant articles and documents

Preparation method for paliperidone palmitate

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.

NOVEL AND IMPROVED 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).

PREPARATION OF PALIPERIDONE

Processes for preparing paliperidone.