CAS: 367514-87-2; Lurasidone

上下游产品

(3aR,7aR)-4'-(benzo[d]isothiazol-3-yl)°Ctahydrospiro[isoindole-2,1'-piperazin]-2-ium methanesulfonate (3aR,4S,7R,7aS)4,7methylene1Hisoindole1,3(2H)-dione bicyclo[2.2.1]heptane-2-exo-3-exodicarboximide (1S,2S)-cyclohexane-1,2-dimethanol bis(methanesulfonate)lurasidone hydr°Chloride (3aR,4S,7R,7aS)-2-(((1R,2R)-2-((4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)methyl)cyclohexyl)methyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione tartrate (3aR,4S,7R,7aS)-2-{(1R,2R)-2-[4-(1,2-benzisothiazol-3-yl)piperazin-1-ylmethyl]cyclohexylmethyl}hexahydro-1H-4,7-methanisoindol-1,3-dione dihydr°Chloride Lurasidone hydr°Chloride

(1R,2R)-(-)-Trans-Cyclohexane-1,2-Dicarboxylic Acid置于甲醇,Sodium Tetrahydroborate,硫酸,四丁基硫酸氢铵,Potassium Carbonate,三乙胺体系中,用 四氢呋喃,二氯甲烷,水,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 13.5H,反应生成 鲁拉西酮
参考文献:一种盐酸鲁拉西酮的制备方法
标题:一种盐酸鲁拉西酮的制备方法
摘要:本发明公开了一种盐酸鲁拉西酮的制备方法,它是以trans-1,2-环己烷二甲酸(Sm-1)为原料经过拆分,甲酯化,还原,甲磺酰化,缩合,重结晶和成盐,最后得到盐酸鲁拉西酮.该方法大大降低了生产成本,具有产品收率高,易于操作,毒性低,适于工业化大规模生产的特点.

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-10005720-B2
优先权日:2013-04-05
标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
发明人：SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

专利号:US-12006301-B1
优先权日:2021-05-13
标题 :And synthesis of dual 5-HT1A and 5-HT7 receptor ligands
发明人：ABLORDEPPEY SETH Y
权利人:FLORIDA A&M UNIV
摘要:Novel dual 5-HT1A and 5-HT7 receptor ligands and methods of using the novel ligands to treat a neurological disorder are presented.

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:US-2018370905-A1
优先权日:2013-04-05
标题:Compounds Useful for the Treatment of Metabolic Disorders and Synthesis of the Same

专利号:US-2012077802-A1
优先权日:2009-06-10
标题 :Histamine h3 inverse agonists and antagonists and methods of use thereof
发明人：CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN
权利人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SUNOVION PHARMACEUTICALS INC
摘要:Provided herein are spiro-cyclic compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.