147663-01-2

Basic information

• Product Name: (S)-9-Hydroxy Risperidone
• Synonyms: (S)-9-Hydroxy Risperidone;(9S)-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;(S)-9-Hydroxy Risperidone ((S)-Paliperidone);Paliperidone S-Isomer;(S)-Paliperidone;Pure Paliperidone (-);9-(S)-Paliperidone;3-[2-[4-(6-Fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9(S)-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one
• CAS NO: 147663-01-2
• 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: 147663-01-2.mol
• Article Data: 61

Chemical Properties

• Appearance: /
• CAS DataBase Reference: (S)-9-Hydroxy Risperidone(CAS DataBase Reference)
• NIST Chemistry Reference: (S)-9-Hydroxy Risperidone(147663-01-2)
• EPA Substance Registry System: (S)-9-Hydroxy Risperidone(147663-01-2)

Safety Data

• Hazardous Substances Data: 147663-01-2(Hazardous Substances Data)

Usage

Uses

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

Upstream product

• 108-20-3 di-isopropyl ether 
• 84163-13-3 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride 
• 108-18-9 diisopropylamine 
• 67-63-0 isopropyl alcohol 
• 1204248-69-0 C₂₃H₂₆FN₅O₃ 
• 106266-06-2 Risperidone 
• 130049-87-5 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-2-methyl-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-ol acetate(ester) 
• 130049-82-0 3-(2-chloroethyl)-9-hydroxy-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one 
• 199739-10-1 paliperidone palmitate 
• 1138463-56-5 3-(2-chloroethyl)-9-oxo-2-methyl-6,7,8,9-tetrahydro-4H-pyrido-[1,2-a]pyrimidin-4-one 
• 147687-17-0 9-(benzyloxy)-3-(2-chloroethyl)-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one 
• 1415488-05-9 3-(2-chloroethyl)-6,7,8,9-tetrahydro-2-methyl-9-hydroxy-4H-pyrido[1,2-a]pyrimidine-4-one palmitate ester 
• 517-23-7 3-acetyl-2-oxo-4,5-dihydrofuran 
• 84163-77-9 6-fluoro-3-(4-piperidinyl)benzo[d]isoxazole 

Downstream Products

• 1172995-13-9 paliperidone stearate 
• 1172995-11-7 paliperidone myristate 

Relevant articles and documents

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.

New synthesis method of paliperidone

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.

A is suitable for industrial production of high-purity 9-hydroxy-risperidone

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.