- Method for preparing lurasidone and salt thereof
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The invention relates to a method for preparing lurasidone and a salt thereof. The method comprises the following steps: reacting (R,R)-1,2-bis(methanesulfonyloxymethyl)cyclohexane and 3-(1-piperazinyl)-1,2-benzoisothiazole hydrochloride in acetonitrile in the presence of potassium carbonate to obtain an intermediate I; reacting the intermediate I with (3aR,4S,7R,7aS)-4,7-methylene-1H-isoindole-1,3(2H)-dione in DMF in the presence of potassium carbonate to prepare lurasidone free alkali; and reacting the lurasidone free alkali with hydrochloric acid in isopropanol to obtain lurasidone hydrochloride. The invention also relates to lurasidone and the salt thereof prepared by using the method, and application of lurasidone and the salt thereof in medicines for resisting psychosis, especially schizophrenia. The method disclosed by the invention has one or more advantages in a group consisting of simple process, high product yield, few impurities and the like.
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- AN IMPROVED PROCESS FOR THE PREPARATION OF LURASIDONE BASE AND ITS SALT
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The present invention relates to an industrially feasible process for preparation of substantially pure Lurasidone base of formula Ia and its conversion to pharmaceutically acceptable salts such as hydrochloride salt and the like in significantly higher yield.
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Paragraph 15
(2017/09/27)
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- Preparation method for lurasidone hydrochloride
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The invention discloses a preparation method for lurasidone hydrochloride. According to the preparation method, trans-1,2-cyclohexanedicarboxylic acid (SM-1) is used as a raw material and subjected to resolution, methyl esterification, reduction, methylsulfonylation, condensation, recrystallization and salt formation so as to eventually obtain lurasidone hydrochloride. The preparation method provided by the invention greatly reduces production cost and has the characteristics of high product yield, easy operation, low toxicity and suitability for industrial large-scale production.
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Paragraph 0035
(2017/08/30)
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- Lurasidone key intermediate preparation method
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The present invention relates to a lurasidone key intermediate preparation method, and belongs to the technical field of compound synthesis. According to the method, when 4,-(1,2-benzisothiazol-3-yl)-(3aR,7aR)-octahydrospiro(2H-isoindole-2,1-piperazine)methanesulfonate is generated, 4-(1,2-benzisothiazol-3-yl)-1-piperazine is adopted as a raw material, the 4-(1,2-benzisothiazol-3-yl)-1-piperazine, (1R,2R)-1,2-bis(methanesulfonyloxymethyl)cyclohexane and potassium carbonate are subjected to a reaction in a solvent toluene, and a cyclodextrin phase transfer catalyst is added to the reaction system. According to the present invention, by using the cyclodextrin as the phase transfer catalyst, the incomplete reaction problem is solved, and the yield is substantially improved.
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Paragraph 0031; 0034
(2017/09/01)
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- Method for preparing lurasidone with high purity and high yield
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The invention provides a method for preparing lurasidone with high purity and high yield. On the basis of an existing lurasidone preparation method, a small quantity of specific protic solvent is added in the preparation process of (R,R)-3a,7a-9H-isoindole-2-1'-[4'-(1,2-benzisothiazole-3-yl)] piperazine mesylate, so that the reaction rate is greatly increased, the time is shortened to 3 h from 23 h in the prior art, the yield is increased from 82% to 90%, the total yield is up to 71%, and the prepared finished product has the consistent quality with original drugs.
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Paragraph 0027; 0029; 0030; 0032; 0034; 0036
(2017/07/21)
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- AN IMPROVED PROCESS FOR THE PREPARATION OF LURASIDONE HYDROCHLORIDE
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Disclosed herein is an improved process for the preparation of Lurasidone and its pharmaceutically acceptable salts via novel intermediate and use thereof for the preparation of an antipsychotic agent useful for the treatment of schizophrenia and bipolar disorder. Further, present invention provides a cost effective and eco-friendly process for producing Lurasidone hydrochloride of formula (I) substantially free of residual solvent(s) at industrial scale.
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Page/Page column 21
(2016/05/24)
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- PROCESS FOR THE INDUSTRIAL SYNTHESIS OF LURASIDONE
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Disclosed is a process for the industrial synthesis of Lurasidone from (1R,2R)-cyclohexane-1,2-diyldimethanol (1), 3-(piperazin-1- yl)benzo[d]isothiazole (3) and (3aR,4R,7R,7aS)-3a,4,7,7a-tetrahydro-4,7- methanoisobenzofuran-1,3-dione (6).). Said process is optimised to obtain Lurasidone with high yields and high purities by preparing highly pure synthesis intermediates, using critical raw materials and reagents in amounts close to the stoichiometric amounts, increasing productivity and reducing the costs and environmental impact of the process.
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- PROCESS FOR LURASIDONE
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The present invention provides a novel process for the purification of lurasidone substantially free of isomeric impurity.
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Page/Page column 5
(2014/07/21)
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- PROCESS FOR THE PREPARATION OF LURASIDONE HYDROCHLORIDE
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The instant invention discloses a process for the preparation of Lurasidone Hydrochloride preparation with lesser impurity profile comprises of isolating Lurasidone base as a solid whereby subjecting the base with isopropyl alcohol-hydrochloric acid.
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Page/Page column 19
(2014/01/09)
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- CRYSTALLINE LURASIDONE HYDROCHLORIDE
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The present invention provides crystalline lurasidone hydrochloride, processes for its preparation, a pharmaceutical composition comprising it and its use for the treatment of schizophrenia.
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Page/Page column 6
(2013/03/28)
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- INTERMEDIATE COMPOUNDS AND PROCESS FOR THE PREPARATION OF LURASIDONE AND SALTS THEREOF
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The present invention relates to a process for the preparation of Lurasidone or a pharmaceutically acceptable salt thereof, a compound useful for the treatment of schizophrenia and bipolar disorder. The present invention further relates to processes for the preparation of Lurasidone intermediates, and to certain novel intermediates obtained by such processes.
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Page/Page column 21
(2013/03/26)
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- NOVEL POLYMORPH OF LURASIDONE HYDROCHLORIDE
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The present invention provides a novel amorphous Form of lurasidone hydrochloride, process for its preparation and pharmaceutical compositions comprising it. In one aspect, the present invention provides an amorphous form of lurasidone hydrochloride. In another aspect, the present invention provides a process for the preparation of lurasidone hydrochloride amorphous Form, which comprises: a) dissolving lurasidone hydrochloride in a mixture of alcoholic solvent and water; and b) subjecting the resulting solution to lyophilization to obtain lurasidone hydrochloride amorphous form.
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Page/Page column 8
(2013/09/26)
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- PROCESS FOR PREPARING BENZISOTHIAZOL-3-YL-PEPERAZIN-L-YL-METHYL-CYCLO HEXYL-METHANISOINDOL-1,3-DIONE AND ITS INTERMEDIATES
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The present invention discloses process for preparing benzisothiazol-3-yl- piperazin-l-yl-methyl-cyclo hexyl-methanisoindol-l,3-dione and intermediates thereof.
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Page/Page column 31
(2013/08/28)
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- PROCESS FOR PRODUCING IMIDE COMPOUND
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The present invention provides an excellent industrial process for producing an imide compound hydrochloride. The process for producing an imide compound hydrochloride of the formula (2): or an enantiomer thereof, which comprises treating a compound of the formula (1): or an enatiomer thereof with an aqueous hydrochloric acid solution in a hydrophilic solvent, followed by crystallizing the resultant.
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Page/Page column 4-7
(2008/06/13)
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