CAS: 87691-87-0; 3-(1-Piperazinyl)-1,2-Benzisothiazole

上下游产品

CAS号110-85-0 哌嗪 | CAS号7716-66-7 3-氯-1,2-苯并异噻唑 | CAS号19602-82-5 2,2-二硫二苯甲酰氯 | CAS号119-80-2 2, 2’-二硫代二苯甲酸(DTSA) | CAS号3950-02-5 Benzoyl chlorid... | CAS号2634-33-5 1,2-苯并异噻唑啉-3-酮 | CAS号105981-34-8 4-[4-(1,2-benzo... | CAS号55745-83-0 2-哌嗪-1-基-1,3-苯并噻唑 | CAS号186204-37-5 (3aR,7aR)-4'-(1... | CAS号131540-88-0 3-piperazin-1-y... | CAS号131779-46-9 1,1-DIMETHYLETH... | CAS号122883-93-6 盐酸齐拉西酮 | CAS号128396-56-5 3-piperazin-1-y... | CAS号118856-18-1 8-((3-(4-(1,2-b...

3-[bis(Hydroxyethyl)]Amino-1,2-Benzisothiazole置于甲基磺酰氯,三乙胺,Ammonium Hydroxide体系中,用 甲醇,乙腈 作为反应溶剂,以71%的收率获得产物3-(1-哌嗪基)-1,2-苯并异噻唑
参考文献: Intermediate Compounds And Process For The Preparation Of Lurasidone And Salts Thereof[fr] Composés Intermédiaires Et Procédé Pour La Préparation De Lurasidone Et De Sels De Celle-Ci
标题: Intermediate Compounds And Process For The Preparation Of Lurasidone And Salts Thereof[fr] Composés Intermédiaires Et Procédé Pour La Préparation De Lurasidone Et De Sels De Celle-Ci

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-11912647-B2
优先权日:2020-05-22
标 题:Diversity-oriented synthesis of N,N,O-trisubstituted hydroxylamines from alcohols and amines by N—O bond formation
发明人：CRICH DAVID; HETTIKANKANAMALAGE ASIRI; HILL JARVIS
权利人:UNIV GEORGIA
摘要:In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.

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-5663449-A
优先权日:1989-05-19
标 题 :Intermediate compounds in the synthesis of heteroarylpiperidines, pyrrolidines and piperazines

专利号:EP-3057966-A1
优先权日:2013-10-17
标 题 :Process for the industrial synthesis of lurasidone

专利号:WO-2015081920-A1
优先权日:2013-12-06
标 题:Process for preparing lurasidone and intermediate thereof
发明人：SLAVIKOVA MARKETA; HAJICEK JOSEF; ZEZULA JOSEF
权利人:ZENTIVA KS
摘要:A new method of synthesis of lurasidone, the substance of the chemical name (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 of structure 1 and its salts. Specifically, a diastereoselective method of preparation of lurasidone based on use of the new intermediate of formula (1)2. The reduction of the nitro group of the intermediate of formula (12) provides the amino intermediate of formula (13), which reacts in the next step with the anhydride of formula (14) with formation of lurasidone of formula (1), which can be further converted to any salt of lurasidone.