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

Description

(S)-9-Hydroxy Risperidone, also known as the S-enantiomer metabolite of Risperidone, is a pharmaceutical compound derived from the metabolism of Risperidone. It acts as a combined serotonin (5-HT2) and dopamine (D2) receptor antagonist, playing a significant role in the treatment of various psychiatric disorders. Its unique properties allow it to modulate neurotransmitter activity, making it a promising candidate for therapeutic applications.

Uses

Used in Pharmaceutical Industry:
(S)-9-Hydroxy Risperidone is used as an active pharmaceutical ingredient (API) for the treatment of psychiatric disorders. Its ability to act as a combined serotonin and dopamine receptor antagonist makes it effective in managing symptoms associated with schizophrenia, bipolar disorder, and other related conditions.
Used in Research and Development:
In the field of pharmaceutical research and development, (S)-9-Hydroxy Risperidone serves as a valuable compound for studying the mechanisms of action and potential applications of Risperidone and its metabolites. This knowledge can be applied to develop new drugs with improved efficacy and safety profiles.
Used in Drug Delivery Systems:
Similar to Gallotannin, (S)-9-Hydroxy Risperidone can also benefit from novel drug delivery systems to enhance its bioavailability, delivery, and therapeutic outcomes. By employing various organic and metallic nanoparticles as carriers, the limitations of (S)-9-Hydroxy Risperidone can be overcome, leading to improved treatment options for patients with psychiatric disorders.

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 
• 199739-10-1 paliperidone palmitate 
• 130049-82-0 3-(2-chloroethyl)-9-hydroxy-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one 
• 1117803-76-5 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-acetyloxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one 
• 1109182-35-5 C₂₈H₃₅FN₄O₄ 
• 1104389-11-8 paliperidone hydrochloride 
• 84163-77-9 6-fluoro-3-(4-piperidinyl)benzo[d]isoxazole 
• 1204248-69-0 C₂₃H₂₆FN₅O₃ 
• 1189516-65-1 R₁₂₅₂₃₉ 
• 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 
• 849727-63-5 (±)-3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one monohydrochloride 

Downstream Products

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

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.

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.