CAS: 14805-29-9; Exo-Hexahydro-1H-4,7-Methanoisoindole-1,3(2H)-Dione

相似化合物

28871-95-6 6713-41-3 1807983-67-0

上下游产品

CAS号14166-28-0 顺式-2,3-降冰片烷二羧酸酐 | CAS号2746-19-2 顺-5-降冰片烯-外型-2,3-二甲酸酐 | CAS号542-92-7 环戊二烯 | CAS号367514-88-3 盐酸鲁拉西酮 | CAS号87760-53-0 坦度螺酮

5-降冰片烯-内-2,3-二甲酰亚胺置于palladium 10% On Activated Carbon,氢气体系中,用 甲醇 用作溶剂,以91.4%的收率获得(3Ar,4S,7R,7As) 4,7-亚甲基-1H-异吲哚-1,3(2H)-二酮
参考文献: Process For The Industrial Synthesis Of Lurasidone[fr] Procédé Pour La Synthèse Industrielle De Lurasidone
标题: Process For The Industrial Synthesis Of Lurasidone[fr] Procédé Pour La Synthèse Industrielle De Lurasidone
摘要:揭示了一种从(1R,2R)-环己烷-1,2-二甲醇(1),3-(哌嗪-1-基)苯并[d]异噻唑(3)和(3Ar,4R,7R,7As)-3A,4,7,7A-四氢-4,7-甲基异苯并呋喃-1,3-二酮(6)合成lurasidone的工业化过程.该过程被优化,通过制备高纯度的合成中间体,使用接近化学计量量的关键原材料和试剂,增加生产率,降低成本并减少环境影响,以高产率和高纯度获得lurasidone.

专利信息

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:ES-2637744-T3
优先权日:2013-10-17
标题 :Process for the industrial synthesis of lurasidone

专利号:CZ-2013977-A3
优先权日:2013-12-06
标题 :Method of lurasidone synthesis