CAS: 130049-82-0; 3-(2-Chloroethyl)-6,7,8,9-Tetrahydro-9-Hydroxy-2-Methyl-4H-Pyrido[1,2-A]Pyrimidine-4-One

上下游产品

CAS号1189516-65-1 帕潘立酮棕榈酸酯氧化杂质 | CAS号144598-75-4 9－羟基利培酮 | CAS号130049-85-3 (R)-9-Hydroxy R... | CAS号199739-10-1 帕潘立酮棕榈酸酯 | CAS号849727-63-5 3-(2-氯乙基)-2-甲基-...

α-乙酰基-γ-丁内酯置于甲烷,三氯氧磷体系中,用 甲醇,甲苯 用作溶剂,55.0 °C,393.01 Kpa 条件下,反应 24.75H,反应生成3-(2-氯乙基)-6,7,8,9-四氢-9-羟基-2-甲基-4H-吡啶并[1,2-A]嘧啶-4-酮
参考文献:3-(2-Chloroethyl)-6,7,8,9-Tetrahydro-9-Hydroxy-2-Methyl-4H-Pyrido[1,2-A]Pyrimidin-4-One 的制备,该合成的关键中间体帕潘立酮
标题:3-(2-Chloroethyl)-6,7,8,9-Tetrahydro-9-Hydroxy-2-Methyl-4H-Pyrido[1,2-A]Pyrimidin-4-One 的制备,该合成的关键中间体帕潘立酮
摘要:需要控制药物产品中的杂质水平,使产品足够纯净,可以安全地用于人体.根据国际协调会议(ich)指南,与药物相关的杂质可分为三大类:有机杂质,无机(元素)杂质和残留溶剂.在这些类别中,基因毒性杂质形成一种特殊情况,即使在低浓度下也会造成重大安全风险.关于基因毒素和基因毒性的定义已经有很多讨论.Ich S2 (R1) 指南将遗传毒性定义为一个广义术语,指的是遗传材料中的任何有害变化.基因毒性杂质也被定义为在适当的测试模型中被证明具有基因毒性的杂质,如艾姆斯细菌基因突变试验.因此,在药物制造中,必须识别,表征,量化和监测杂质.显然,杂质包括那些甚至可能存在于起始材料中的杂质,这些杂质来自多步合成序列中的副反应和/或与溶剂和试剂的相互作用.本文介绍了一种制备 3-(2-氯乙基)-6,7,8,9-四氢-9羟基-2-甲基-4H-吡啶并[1,2-A]嘧啶-4的改进和有效方法-One (4A),合成帕潘立酮的关键中间体.鉴于
Doi:10.1080/00304948.2016.1165060

专利信息

专利号:WO-2010064134-A3
优先权日:2008-12-05
标 题:Process of synthesis of paliperidone
发明人：MODI INDRAVADAN AMBALAL; SODAGAR KEVAL RAMESHCHANDRA; VINEET MALIK; JAIN SUDHIR HUKAMCHAND; PARIKH SANJAY NATVARLAL; SHARMA ARUN OMPRAKASH; BAPAT UDAY RAJARAM; KHAMAR BAKULESH MAFATLAL
权利人:CADILA PHARMACEUTICALS LTD; MODI INDRAVADAN AMBALAL; SODAGAR KEVAL RAMESHCHANDRA; VINEET MALIK; JAIN SUDHIR HUKAMCHAND; PARIKH SANJAY NATVARLAL; SHARMA ARUN OMPRAKASH; BAPAT UDAY RAJARAM; KHAMAR BAKULESH MAFATLAL
摘要:The invention relates to an improved process for preparation of 3-(2-chloroethyl)-9-hydroxy-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one, an intermediate used in the synthesis of paliperidone and process for converting the same to Paliperidone.

专利号:US-7977480-B2
优先权日:2007-12-10
标 题:Synthesis of paliperidone
发明人：BARTL JIRI; KRAJCOVIC JOZEF; BENOVSKY PETR
权利人:SYNTHON BV
摘要:A 9-hydroxy or 9-acyloxy group can be added to a pyridopyrimidinone ring structure by a process comprising acylating a compound of formula (5) under Vilsmeier-Haack or Friedel-Crafts conditions to form a compound (6); and transforming with a peroxo-compound to obtain the compound (1). n nR represents hydrogen or a C1-C20 acyl group. The process is useful in the synthesis of paliperidone and derivatives.

专利号:EP-2454256-B1
优先权日:2009-07-13
标题 :Process for the synthesis of paliperidone
发明人：RUZIC MILOS; PECAVAR ANICA; PRUDIC DARJA; PLAPER IGOR; KLOBCAR ANDREJ; PLEVNIK MIHA; HVALA JERNEJ
权利人:KRKA D D NOVO MESTO
摘要:The invention describes an improved process for the synthesis and purification of paliperidone.

专利号:US-2008214809-A1
优先权日:2006-08-23
标 题 :Process for the synthesis of CMHTP and intermediates thereof
发明人：DOLITZKY BEN-ZION; SHAPIRO EVGENY; INI SANTIAGO; SHMUELY YARON; LANCRY ELI; PILARSKY GIDEON
权利人:DOLITZKY BEN-ZION; SHAPIRO EVGENY; INI SANTIAGO; SHMUELY YARON; LANCRY ELI; PILARSKY GIDEON
摘要:The present invention provides processes of preparing 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]-pyrimidin-4-one (CMHTP) useful as intermediates for the preparation of paliperidone, wherein the processes use 3-(2-chloroethyl)-2-methyl-9-benzyloxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMBP) and/or 3-(2-chloroethyl)-2-methyl-9-hydroxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMHP) having phosphorus at least partially removed as the intermediate.

专利号:US-7820816-B2
优先权日:2006-08-23
标题:Process for the synthesis of CMHTP and intermediates thereof
发明人：DOLITZKY BEN-ZION; SHAPIRO EVGENY; INI SANTIAGO; SHMUELY YARON; LANCRY ELI
权利人:TEVA PHARMA
摘要:The present invention provides 3-benzyloxy-2-aminopyridine (BOPA), 3-(2-Hydroxyethyl)-2-methyl-9-hydoxy-4H-pyrido[1,2-a]pyrimidine-4-one (HMBP), 3-(2-Chloroethyl)-2-methyl-9-hydoxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMHP) and 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]-pyrimidin-4-one (CMHTP) useful as intermediates for the preparation of paliperidone. The present invention also provides processes for preparing these intermediates and for preparing paliperidone.

专利号:US-2011087024-A1
优先权日:2008-04-21
标题:process for the preparation of paliperidone intermediates
发明人：PRABAHAR KOILPILLAI JOSEPH; KULKARNI PRAVIN BHALCHANDRA; KELKAR LAXMIKANT MADHUKAR; KALE SANJAY ANANTHA; POTDAR SHASHANK GOPAL; NARWADE KRISHNA BABAN; KHAN MUBEEN AHMED; THORAT JITENDRA RAMAKANT
权利人:GLENMARK HOUSE
摘要:The present invention relates to a process for the preparation of 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]-pyrimidin-4-one; and its use in the synthesis of paliperidone.