- Preparation method of carlyrazide and intermediate compound
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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.
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- Preparation method of carbaprizine
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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.
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- Cariprazine synthesis method
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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%.
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Paragraph 0017; 0024-0035
(2020/03/17)
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- 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
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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.
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- A PROCESS FOR THE PREPARATION OF CARIPRAZINE HYDROCHLORIDE
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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
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Page/Page column 12-13
(2019/06/17)
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- Preparation method of cariprazine
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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.
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- Method for preparing medicinal carliflazine composition
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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
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- D2 Dopamine Receptor G Protein-Biased Partial Agonists Based on Cariprazine
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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
- Shen, Yudao,McCorvy, John D.,Martini, Michael L.,Rodriguiz, Ramona M.,Pogorelov, Vladimir M.,Ward, Karen M.,Wetsel, William C.,Liu, Jing,Roth, Bryan L.,Jin, Jian
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p. 4755 - 4771
(2019/05/08)
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- Novel method for synthesizing cariprazine
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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.
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- 3 - cyclohexyl - 1, 1 - dimethyl urea compound and its preparation method and application
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The invention discloses a 3-cyclohexyl-1,1-dimethylurea compound as well as a preparation method and application thereof. The 3-cyclohexyl-1,1-dimethylurea compound is used for preparing an antischizophrenic drug cariprazine. Compared with the prior art and report literatures, the preparation method of the 3-cyclohexyl-1,1-dimethylurea compound has the remarkable advantages of being free of removal of protecting groups such as Boc group, high in atom economy, low in cost and easy in getting of raw materials, mild in reaction condition, stable in yield, simple and convenient to operate, controllable in product quality, high in product purity, less in three waste pollution and easy to produce industrially. The structure formula of the 3-cyclohexyl-1,1-dimethylurea compound is as shown in (I) in the specification.
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- Compound for preparation of cariprazine and preparation method thereof
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The invention relates to a compound for preparation of cariprazine and a preparation method thereof. The method can overcome the defects in the prior art, the used raw materials and reagents are low toxic, cheap and easily available, the reaction conditions are mild, fewer three wastes are generated, at the same time, the operation is simple and safe, and the yield is good, therefore the method is suitable for industrialized production.
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- Preparation method of cariprazine
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The invention discloses a preparation method of cariprazine (Cariprazine, RGH 188). The method includes the preparation steps of preparing 4-[2-[4-(2,3-dichlorophenyl)piperazine]-1-based]ethyl]cyclohexanone by making 4-(2-hydroxyethyl)cyclohexanone and 1-(2,3-dichlorophenyl)piperazine subjected to a condensation reaction, preparing trans-4-[[2-]4-(2,3-dichlorophenyl)piperazine]-1-based]ethyl]cyclohexylamine by making the obtained intermediate subjected to a reduction ammonolysis reaction, and preparing cariprazine by making the intermediate and N,N-dimethylcarbamyl chloride subjected to an acylation reaction. According to the preparation method, raw materials can be easily obtained, the process is simple, and the method is economical, environmentally friendly and suitable for industrialized production.
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- A structure-activity analysis of biased agonism at the dopamine D2 receptor
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Biased agonism offers an opportunity for the medicinal chemist to discover pathway-selective ligands for GPCRs. A number of studies have suggested that biased agonism at the dopamine D2 receptor (D2R) may be advantageous for the treatment of neuropsychiatric disorders, including schizophrenia. As such, it is of great importance to gain insight into the SAR of biased agonism at this receptor. We have generated SAR based on a novel D2R partial agonist, tert-butyl (trans-4-(2-(3,4-dihydroisoquinolin- 2(1H)-yl)ethyl)cyclohexyl)carbamate (4). This ligand shares structural similarity to cariprazine (2), a drug awaiting FDA approval for the treatment of schizophrenia, yet displays a distinct bias toward two different signaling end points. We synthesized a number of derivatives of 4 with subtle structural modifications, including incorporation of cariprazine fragments. By combining pharmacological profiling with analytical methodology to identify and to quantify bias, we have demonstrated that efficacy and biased agonism can be finely tuned by minor structural modifications to the head group containing the tertiary amine, a tail group that extends away from this moiety, and the orientation and length of a spacer region between these two moieties.
- Shonberg, Jeremy,Herenbrink, Carmen Klein,López, Laura,Christopoulos, Arthur,Scammells, Peter J.,Capuano, Ben,Lane, J. Robert
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p. 9199 - 9221
(2014/01/06)
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- NOVEL PROCESS FOR THE PREPARATION OF PIPERAZINE COMPOUNDS AND HYDROCHLORIDE SALTS THEREOF
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The invention relates to a new process for the preparation of compounds of general formula (I) wherein R1 and R2 represent independently hydrogen or C1-6 alkyl with straight or branched chain optionally substituted with ar
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Page/Page column 10
(2011/07/07)
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