CAS: 119532-26-2; 1-(2,3-Dichlorophenyl)Piperazine Hydrochloride

2,3-二氯溴苯置于盐酸,Tris-(Dibenzylideneacetone)Dipalladium(0),Potassium Carbonate,2-二环己基磷-2,4,6-三异丙基联苯体系中,用 乙腈 用作溶剂,化学反应 8.0H,反应生成1-(2,3-二氯苯基)哌嗪
参考文献:氘代阿立哌唑及其制备方法和用途
标题:氘代阿立哌唑及其制备方法和用途
摘要:本发明属于有机和药物合成领域,公开一种氘代d8阿立哌唑及其制备方法和应用,该方法以1,4‑二氯丁烷‑d8为原料,经四步反应合成得到氘代标记d8‑阿立哌唑;本发明所提供的制备方法,整个工艺设计合理,可操作性强,操作简单,氘代试剂成本低,产物容易分离纯化,所得目标产物化学性质稳定,同位素丰度高,收率高,纯度可达100%.本发明制备方法可用于生产分析检测氘代阿立哌唑时使用的氘代内标物,可为阿立哌唑代谢机理研究提供试样品,从而更加准确和方便地了解阿立哌唑在人体内的代谢过程和作用机制;可制备药物组合物,用于多巴胺系统稳定剂-治疗精神分裂症,分裂情感性精神病和其他精神病性障碍等,具有重要的应用价值.

专利信息

专利号:US-2007149782-A1
优先权日:2005-12-23
标 题:Methods of preparing a crystalline form of 7-(4-chlorobutoxy)-3,4-dihydro-2(1h)-quinolinone and the use thereof in the synthesis of Aripiprazole
发明人：BRAND MICHAEL; SHOOKRUN MOTY; GRIBUN IRINA; ADIN ITAI; IUSTAIN CARMEN; BRAVERMAN OLEG; UDIS NATALIA; ARAD ODED; KASPI JOSEPH
权利人:BRAND MICHAEL; SHOOKRUN MOTY; GRIBUN IRINA; ADIN ITAI; IUSTAIN CARMEN; BRAVERMAN OLEG; UDIS NATALIA; ARAD ODED; KASPI JOSEPH
摘要:The present invention relates to methods of preparing a highly pure crystalline form of 7-(4-chlorobutoxy)-3,4-dihydro-2(1H)-quinolinone, which is a chemical intermediate useful in the preparation of Aripiprazole thereof in high quality and yield, and provides data that characterizes the crystalline form of 7-(4-chlorobutoxy)-3,4-dihydro-(1H)-quinolinone.

专利号:US-9795685-B2
优先权日:2012-08-21
标 题 :Haptens of aripiprazole
发明人：LIN RONGHUI; SALTER RHYS; DECORY THOMAS R; HRYHORENKO ERIC; REMMERIE BART M; SANKARAN BANUMATHI
权利人:JANSSEN PHARMACEUTICA NV
摘要:The invention relates to compounds of Formula I, wherein R 1 , R 2 , and R 3 are defined in the specification, useful for the synthesis of novel conjugates and immunogens derived from aripiprazole. The invention also relates to conjugates of an aripiprazole hapten and a protein.

专利号:US-2005215791-A1
优先权日:2004-02-05
标题:Process for preparing aripiprazole
发明人：DOLITZKY BEN-ZION; LERMAN ORI
权利人:DOLITZKY BEN-ZION; LERMAN ORI
摘要:The invention encompasses the synthesis of aripiprazole from BBQ and DCP, and comprises mixing 7-(4-bromobutoxy)-3,4-dihydrocarbostyril (BBQ) and 1-(2,3-dichlorophenyl)piperazine hydrochloride (DCP) in the presence of at least one base and at least one organic solvent to form a reaction mixture; heating the reaction mixture for a sufficient amount of time to effect the reaction; and isolating aripiprazole. The invention also encompasses the use of phase transfer catalysts in synthesizing aripiprazole from BBQ and DCP.

专利号:CN-1513838-A
优先权日:2003-08-08
标题:One-pot synthesis of aripiprazole

专利号:CN-113214150-A
优先权日:2021-04-20
标 题:A kind of synthesis of high-purity aripiprazole and preparation method of hydrate microparticles

专利号:CN-1263740-C
优先权日:2003-08-08
标 题 :One-pot synthesis of aripiprazole