186204-35-3Relevant articles and documents
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.
A process for the preparation of intermediates [...] (by machine translation)
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Paragraph 0008, (2017/01/09)
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)
PROCESS FOR THE INDUSTRIAL SYNTHESIS OF LURASIDONE
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Page/Page column 14, (2015/05/05)
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.