1318074-25-7Relevant articles and documents
Preparation method of lurasidone
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Paragraph 0032-0046, (2021/07/31)
The invention relates to a preparation method of lurasidone. The preparation method comprises the following steps of: reacting a compound as shown in a formula (I) with a compound as shown in a formula (II) under the action of an organic solvent A and a catalyst A, and performing quenching with a weak base solution to obtain a lurasidone crude product. According to the preparation method, the organic solvent A is selected from N-methyl pyrrolidone, N, N-dimethylformamide or a mixture of N-methyl pyrrolidone and N, N-dimethylformamide, preferably N-methyl pyrrolidone; the catalyst A is cesium carbonate; the weak base solution is selected from a cesium carbonate solution, a potassium carbonate solution or a sodium carbonate solution, preferably the potassium carbonate solution. The method is simple to operate, high in product yield, short in reaction time, low in cost and suitable for actual industrial production.
Method for preparing lurasidone and salt thereof
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, (2020/02/10)
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.
Preparation of west lulalula alkone isomer impurities (by machine translation)
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Paragraph 0016, (2019/04/26)
West hydrochloric acid lulalula alkone, chemical name: (3 aR, 4S, 7R, 7 AS) - 2 - {(1R, 2R) - 2 - [4 - (1, 2 - Benzothiazole - 3 - yl) piperazine - 1 - yl methyl] cyclohexyl methyl} hexahydro - 1H- 4, 7 - Methyl isobutyl ketone indole - 1, 3 - dione hydro
Preparation method for lurasidone hydrochloride
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, (2017/08/30)
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.
Lurasidone key intermediate preparation method
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Paragraph 0031; 0033, (2017/09/01)
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.
AN IMPROVED PROCESS FOR THE PREPARATION OF LURASIDONE BASE AND ITS SALT
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Page/Page column 13-14, (2017/09/27)
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.
A method for preparing [...]
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Paragraph 0041; 0055-0063, (2018/02/04)
The invention provides a method for preparing lurasidone. The preparation method comprises reacting 1-(1,2-benzisothiazol-3-yl) piperazine with (R, R)-1,2-bis(methylsulfonyl-methoxy) cyclohexane in a mixed solvent of acetonitrile/water in presence of bicarbonate as a base, adding toluene or xylene, separating an organic layer out, adding bicyclo [2.2.1] heptane-2,3-dicarboximide and carbonate into the organic layer and reacting to obtain lurasidone. The conventional separation and purification steps are omitted and the cost of production is greatly reduced; at the same time, the method has the characteristics of high yield and high purity of the product.
Method for preparing lurasidone with high purity and high yield
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, (2017/07/21)
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.
AN IMPROVED PROCESS FOR THE PREPARATION OF LURASIDONE HYDROCHLORIDE
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Page/Page column 21, (2016/05/24)
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.
PROCESSES FOR MAKING ALKYLATED ARYLPIPERAZINE AND ALKYLATED ARYLPIPERIDINE COMPOUNDS INCLUDING NOVEL INTERMEDIATES
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, (2015/12/30)
Novel processes, and intermediates, for making alkylated arylpiperazine and alkylated arylpiperidine compounds of the general formulas (I) and (VII), respectively wherein, R1 and R2 are individually selected from hydrogen, alkyl, sub