专利号:US-9518047-B2 优先权日:2013-10-17 标题 :Process for the industrial synthesis of lurasidone 发明人:ANGELINI TOMMASO; BETTONI PIERGIORGIO; ROLETTO JACOPO; PAISSONI PAOLO 权利人:PROCOS SPA 摘要: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.
专利号:US-10196400-B2 优先权日:2015-01-08 标 题:Process for the preparation of lurasidone and its intermediate 发明人:GHARPURE MILIND; TIWARI SHASHI KANT; WAGH GANESH; REVANAPPA GALGE; WARPE MANIKRAO; ZALTE YOGESH; KRISHNMURTHY DHILEEPKUMAR 权利人:PIRAMAL ENTPR LTD 摘要:The present invention provides an improved process for preparation of the substantially pure (3aR,7aR)-4′-(benzo[d]isothiazol-3-yl)octahydrospiro[isoindole-2,1′-piperazin]-1′-ium methanesulfonate (referred to as compound-II), which is useful as a key intermediate for the synthesis of lurasidone ((3aR,4S,7R,7aS)-2-{(1R,2R)-2-[4-(1,2-benzisothiazol-3-yl)piperazin-1ylmethyl]cyclohexylmethyl}hexahydro-4,7-methano-2H-isoindole-1,3-dione). The process comprises reaction of the compound-III (as described herein) with the compound-IV (as described herein) in the presence of a solvent mixture selected from an alcohol and water; and a base The improved process for the preparation of compound II provides the product with total amount of unreacted compound-IV as impurity in less than 0.06% and the product with HPLC purity as ≥99.8%. The process further refers purification of Lurasidone hydrochloride, wherein the product contains the residual acetone <5000 ppm.
专利号:JP-2016533359-A 优先权日:2013-10-17 标题:Process of industrial synthesis of lurasidone
专利号:US-8853395-B2 优先权日:2013-02-22 标 题 :Process for the preparation of lurasidone hydrochloride 发明人:ZACCHE MATTEO; Gerli Fulvio; GATTI PIERANDREA 权利人:EDMOND PHARMA SRL 摘要:Disclosed is a new and efficient process for the synthesis with high yields and purity of lurasidone hydrochloride, a medicament which is useful as a psychotropic substance. The process involves the preparation of lurasidone base in a reaction system not containing inorganic salts, followed by conversion of the latter to an addition salt with an organic carboxylic acid, which is finally converted to lurasidone hydrochloride.
专利号:IT-MI20131737-A1 优先权日:2013-10-17 标 题 :PROCESS FOR THE INDUSTRIAL SYNTHESIS OF LURASIDONE
专利号:ES-2637744-T3 优先权日:2013-10-17 标题 :Process for the industrial synthesis of lurasidone