839712-12-8

Basic information

• Product Name: Cariprazine
• Synonyms: Urea, N'-[trans-4-[2-[4-(2,3-dichlorophenyl)-1-piperazinyl]ethyl]cyclohexyl]-N,N -diMethyl-;Cariprazine;N'-[trans-4-[2-[4-(2,3-Dichlorophenyl)-1-piperazinyl]ethyl]cyclohexyl]-N,N-dimethylurea;RGH 188
• CAS NO: 839712-12-8
• Molecular Formula: C₂₁H₃₂Cl₂N₄O
• Molecular Weight: 427.41098
• EINECS: 1592732-453-0
• Product Categories: Aromatics;Heterocycles;Intermediates & Fine Chemicals;Neurochemicals;Pharmaceuticals;Inhibitor;CARIPRAZINE and Impurities
• Mol File: 839712-12-8.mol

Chemical Properties

• Appearance: /
• Density: 1.24
• Storage Temp.: -20°C Freezer, Under inert atmosphere
• Solubility: DMSO (Slightly), Methanol (Slightly)
• CAS DataBase Reference: Cariprazine(CAS DataBase Reference)
• NIST Chemistry Reference: Cariprazine(839712-12-8)
• EPA Substance Registry System: Cariprazine(839712-12-8)

Safety Data

• Hazardous Substances Data: 839712-12-8(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
Cariprazine is used as an antipsychotic drug for the treatment of schizophrenia, bipolar mania, and depression due to its D2/D3 dopamine receptor antagonist properties.

Upstream product

• 32863-01-7 4-(2-hydroxyethyl)cyclohexan-1-one 
• 41202-77-1 1-(2,3-dichlorophenyl)piperazine 
• 87976-86-1 4‐aminocyclohexanone 
• 119532-26-2 1-(2,3-dichlorophenyl)-piperazine hydrochloride 
• 1313279-47-8 trans-(4-cyanomethyl-cyclohexyl)-carbamic acid tert-butyl ester 
• 239074-29-4 trans (4-hydroxymethyl-cyclohexyl)-carbamic acid tert-butyl ester 
• 27960-59-4 trans-4-aminocyclohexanecarboxylic acid hydrochloric acid 
• 146307-51-9 methyl (1R,4R)-4-((tert-butoxycarbonyl)amino)cyclohexane-1-carboxylate 
• 791778-53-5 trans-4-(2-(4-(2,3-dichlorophenyl)piperazin-1-yl)ethyl)cyclohexane-1-amine 
• 27514-08-5 N-(4-oxocyclohexyl)acetamide 
• 2901-44-2 trans-2-(4-acetamidocyclohexyl)acetic acid 

Downstream Products

• 1083076-69-0 Cariprazine hydrochloride 

Relevant articles and documents

Preparation method of carlyrazide and intermediate compound

The present invention provides a method for preparing carlirazine and an intermediate compound. The preparation method of the present invention is simple, no need for high temperature and high pressure conditions and the use of a precious catalyst, cost savings, and the yield and purity of carilazine are high.

Preparation method of carbaprizine

The invention discloses a preparation method of carbaprizine. The novel intermediate and provided by the invention is a method for preparing carbapine from the intermediate, and the method avoids the use of the gene toxic impurity dimethyl carbamoyl chloride, and is good in safety, ideal in product yield and purity and suitable for industrial production.

Cariprazine synthesis method

The invention provides a cariprazine synthesis method, which comprises the following steps: carrying out acylation on a compound (I) in a reaction solvent with a proper temperature and dimethylaminoformyl chloride into an aqueous solution of an inorganic alkali to obtain cariprazine (compound II), wherein the reaction formula is defined in the specification. According to the invention, the synthesis method overcomes the defects of long reaction time, large impurity, difficulty in purification and the like in the prior art, and provides a novel method with characteristics of rapid reaction, small impurity, easy purifying, high yield and suitable for commercial mass production, wherein the purity of the product can reach more than 99.0%.

Method for preparing medicinal carliflazine composition

The invention provides a medicinal high-purity carliflazine composition and a method for preparing the medicinal high-purity carliflazine composition. The preparation process of the medicinal carliprazine composition can obviously reduce the content of mo

D2 Dopamine Receptor G Protein-Biased Partial Agonists Based on Cariprazine

Functionally selective G protein-coupled receptor ligands are valuable tools for deciphering the roles of downstream signaling pathways that potentially contribute to therapeutic effects versus side effects. Recently, we discovered both Gi/o-bi

A PROCESS FOR THE PREPARATION OF CARIPRAZINE HYDROCHLORIDE

The present invention is directed towards a process for the preparation of Cariprazine (Ia) or a pharmaceutically acceptable salt thereof, wherein, N,N- dimethyl-1H-imidazole-1-carboxamide alkyl halide (VII) is reacted with trans-4- (2-(4-(2,3-dichlorophe

NOVEL PROCESSES FOR THE PREPARATION OF TRANS-N-{4-[2-[4-(2,3-DICHLOROPHENYL)PIPERAZINE-1-YL]ETHYL] CYCLOHEXYL}-N',N'-DIMETHYLUREA HYDROCHLORIDE AND POLYMORPHS THEREOF

The present invention relates to novel processes for the preparation of trans- N-{4-[2- [4-(2,3-dichloro phenyl) piperazine-1-yl] ethyl] cyclohexyl} -N',N'-dimethylurea hydrochloride represented by the following structural formula-1a and polymorphs thereof. (I) The present invention also relates to novel intermediate compounds which are useful for the preparation of compound of formula-1a.

Preparation method of cariprazine

The invention provides a preparation method of cariprazine. The preparation method of the cariprazine includes that a trans-2-(trans-4-(3, 3-dimethylureido) cyclohexyl) derivative is enabled to reactwith 1-(2, 3-dichlorophenyl) piperazine or salt thereof in an acid-binding agent reaction condition, and then the cariprazine is generated in a reducing agent reaction condition. The preparation method of the cariprazine is few in a synthetic route, simple in technology and conformable to production requirements.

Novel method for synthesizing cariprazine

The invention belongs to the technical field of organic synthesis, and provides a novel method for synthesizing cariprazine. The novel method comprises the following steps: firstly, carrying out condensation reaction on trans-2-(4-(3,3-dimethyl ureido) cyclohexyl) acetic acid and 1-(2,3-dichlorophenyl) piperazine to obtain 3-(trans-4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-2-oxo-ethyl}-cyclohexyl)-1,1-dimethylurea; and secondly, reducing 3-(trans-4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-2-oxo-ethyl}-cyclohexyl)-1,1-dimethylurea by using borane to obtain the cariprazine. The method hasthe advantages that process steps are greatly shortened, the purity of a final product is ensured and the total yield is obviously increased.