- 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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- 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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- A process for the preparation of intermediates [...] (by machine translation)
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The invention relates to a process for the preparation of intermediates [...], the intermediate body is (3aR, 7aR) - 4 ˊ - (1,2-benzisothiazol-3-yl) eight hydrogen spiral [2H-isoindole -2,1 ˊ-piperazine] a sulfonate. The (1R, 2R) - 1,2-cyclohexane dimethanol as raw materials, dialkyltinacetal after armor is a sulfonic acid ester, with the 3 - (1-piperazinyl) - 1,2 benzothiazin hydrochloride reaction to obtain the required intermediate. (by machine translation)
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Paragraph 0008
(2017/01/09)
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- Enantioselective Synthesis of ((1 R,2 R)-Cyclohexane-1,2-diyl)bis(methylene)dimethanesulfonate, a Lurasidone Hydrochloride Intermediate
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A concise, economical, and highly enantioselective synthesis of bismesylate intermediate of lurasidone HCl, an antipsychotic, has been developed. The key steps involved in the synthesis are thionyl chloride-catalyzed esterification of tetrahydrophthalic anhydride in MeOH, epimerization of cis to trans isomer, hydrolysis of the diester, resolution of the diacid, reduction with Red-Al, and finally bismesylation of the corresponding diol, which provided the desired intermediate ((1 R,2 R)-cyclohexane-1,2-diyl)bis(methylene) dimethanesulfonate in overall good yield.
- Ravi Ganesh,Pachore, Sharad S.,Pratap,Umesh,Basaveswara Rao,Murthy,Suresh Babu
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p. 2676 - 2682
(2015/12/18)
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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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Page/Page column 14
(2015/05/05)
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- PROCESS FOR THE PREPARATION OF LURASIDONE HYDROCHLORIDE
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Provided herein is a process for the preparation of the antipsychotic agent lurasidone hydrochloride useful for the treatment of schizophrenia.
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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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- 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 12
(2014/01/09)
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- PROCESS FOR THE PREPARATION OF AN ANTIPSYCHOTIC AGENT
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The present invention provides a process for the preparation of an antipsychotic agent useful for the treatment of schizophrenia.
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Page/Page column 14
(2012/10/18)
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