CAS: 144598-75-4; 3-(2-(4-(6-Fluorobenzo[d]Isoxazol-3-yl)Piperidin-1-yl)Ethyl)-9-Hydroxy-2-Methyl-6,7,8,9-Tetrahydro-4H-Pyrido[1,2-A]Pyrimidin-4-One

上下游产品

di-isopropyl ether 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydr°Chloride diisopropylamine isopropyl alcoholpaliperidone myristate paliperidone stearate paliperidone palmitate 3-{2-[4-(4-fluoro-2-hydroxybenzoyl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one

帕潘立酮棕榈酸酯置于盐酸体系中,用 水 用作溶剂,化学反应 2.0H,以90%的收率获得帕潘立酮
参考文献:Preparation Of 3-[2-[4-((6-Fluoro-1,2-Benzisoxazol-3-yl)-L-Piperidinyl)-6,7,8,9-Tetrahydro-9-Hydroxy-2-Methyl-4H-Pyrido[ 1,2-A]-Pyrimidin-4-One (Paliperidone) And Paliperidone Palmitate.
标题:Preparation Of 3-[2-[4-((6-Fluoro-1,2-Benzisoxazol-3-yl)-L-Piperidinyl)-6,7,8,9-Tetrahydro-9-Hydroxy-2-Methyl-4H-Pyrido[ 1,2-A]-Pyrimidin-4-One (Paliperidone) And Paliperidone Palmitate.
摘要:一种改进的合成过程,用于合成3-[2-[4-((6-氟-1,2-苯并异噁唑-3-基)-1-哌啶基]-6,7,8,9-四氢-9-羟基-2-甲基-4H-吡啶并[1,2-A]-嘧啶-4-酮(帕利哌酮)和帕利哌酮棕榈酸酯,通过一种新颖的中间体(2-氯乙基)-6,7,8,9-四氢-2-甲基-9-羟基-4H-吡啶并[1,2-A]嘧啶-4-酮棕榈酸酯.

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.