CAS: 260273-82-3; 3-(2-Chloroethyl)-9-Hydroxy-2-Methyl-4H-Pyrido[1,2-A]Pyrimidin-4-One

上下游产品

3-acetyl-2-oxo-4,5-dihydrofuran 2-amino-3-benzyloxypyridine 2-amino-3-hydroxypyridine 9-(benzyloxy)-3-(2-chloroethyl)-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-acetyloxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one 3-(2-chloroethyl)-9-hydroxy-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one paliperidone

α-乙酰基-γ-丁内酯置于氢气,钯,三氯氧磷体系中,用 甲苯 用作溶剂,化学反应生成3-(2-氯乙基)-2-甲基-9-羟基-4H-吡啶并[1,2A]嘧啶-4酮 (帕潘立酮)
参考文献:Methods And Compositions For Treatment Of Cancer
标题:Methods And Compositions For Treatment Of Cancer
摘要:在某个方面,该披露涉及angptl4的抑制剂;制备所述化合物的合成方法;包括所述化合物的药物组合物;治疗细胞不受控制增殖的疾病的方法,例如癌症;以及使用所述化合物和药物组合物治疗与angptl4功能障碍相关的疾病的方法.本摘要旨在作为在特定领域搜索的扫描工具,并不打算限制本披露.

专利信息

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: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.

专利号:US-8940749-B2
优先权日:2011-05-31
标题:Preparation of 3-[2-[4-((6-fluoro-1, 2-benzisoxazol-3-yl)-l-piperidinyl)-6, 7, 8, 9-tetrahydor-9-hydroxy-2-methyl-4H-pyrido[ 1, 2-A]-pyrimidin-4-one(paliperidone) and paliperidone palmitate
发明人：DAVULURI RAMAMOHAN RAO; PONNAIAH RAVI; NEELA PRAVEEN KUMAR; BATTHINI GURUSWAMY; VENKATA NARASIMHARAO TELAGAREDDY; RAVANABABU KOSIREDDY; SUDHEER KALLEPALLY
权利人:DAVULURI RAMAMOHAN RAO; PONNAIAH RAVI; NEELA PRAVEEN KUMAR; BATTHINI GURUSWAMY; VENKATA NARASIMHARAO TELAGAREDDY; RAVANABABU KOSIREDDY; SUDHEER KALLEPALLY
摘要:An improved process for the synthesis of 3-[2-[4-((6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]-pyrimidin-4-one (Paliperidone) and Paliperidone Palmitate through a novel intermediate (2-Chloroethyl)-6,7,8,9-tetrahydro-2-methyl-9-hydroxy-4H-pyrido [1,2-a]pyrimidine-4-one Palmitate ester.

专利号:WO-2009074333-A1
优先权日:2007-12-10
标 题 :Synthesis of paliperidone