CAS: 199739-10-1; 3-(2-(4-(6-Fluorobenzo[d]Isoxazol-3-yl)Piperidin-1-yl)Ethyl)-2-Methyl-4-Oxo-6,7,8,9-Tetrahydro-4H-Pyrido[1,2-A]Pyrimidin-9-Yl Palmitate

上下游产品

1-hexadecylcarboxylic acid paliperidone n-hexadecanoyl chloride palmitic anhydridepaliperidone 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7-dihydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-2-methyl-9-pentadecyl-4H-pyrido[1,2-a]pyrimidin-4-one

棕榈酸置于4-二甲氨基吡啶,Potassium Carbonate,三乙胺体系中,用 二氯甲烷,乙腈 用作溶剂,化学反应 17.42H,反应生成帕潘立酮棕榈酸酯
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.[fr] Préparation De 3-[2-[4-((6-Fluoro-1,2-Benzisoxazol-3-yl)-L-Pipéridinyl)-6,7,8,9-Tétrahydro-9-Hydroxy-2-Méthyl-4H-Pyrido [ 1,2-A]-Pyrimidin-4-One (Palepéridone) Et De Palmitate De Palipéridone
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.[fr] Préparation De 3-[2-[4-((6-Fluoro-1,2-Benzisoxazol-3-yl)-L-Pipéridinyl)-6,7,8,9-Tétrahydro-9-Hydroxy-2-Méthyl-4H-Pyrido [ 1,2-A]-Pyrimidin-4-One (Palepéridone) Et De Palmitate De Palipéridone
摘要:提供一种合成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的过程,通过一种新颖的中间体3-(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.还提供了一种通过化合物vii合成化合物viii的方法.

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-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-2010003702-A9
优先权日:2008-07-11
标题:Synthesis of paliperidone

专利号:ES-2436658-T3
优先权日:2007-12-10
标题 :Synthesis of paliperidone

专利号:US-2009156810-A1
优先权日:2007-12-10
标 题:Synthesis of paliperidone

专利号:US-2010010218-A1
优先权日:2008-07-11
标题 :Synthesis of paliperidone