CAS: 63234-80-0; 3-(2-Chloroethyl)-2-Methyl-6,7,8,9-Tetrahydro-4H-Pyrido[1,2-A]Pyrimidin-4-One

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130049-82-0 93076-03-0 63234-80-0

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CAS号41078-70-0 3-(2-氯乙基)-2-甲基-... | CAS号504-29-0 2-氨基吡啶 | CAS号517-23-7 2-乙酰基-γ-丁内酯 | CAS号380634-63-9 3-(1-(pyridin-2... | CAS号106266-06-2 利培酮

α-乙酰基-γ-丁内酯置于palladium On Activated Charcoal,氢气,三氯氧磷体系中,用 乙醇,甲苯 作为反应溶剂,化学反应 26.0H,反应生成 3-(2-氯乙基)-6,7,8,9-四氢-2-甲基-4H-吡啶并[1,2-A]嘧啶-4-酮
参考文献:消除杂环正电子发射断层扫描放射性配体的铜介导的 18F-氟化
标题:消除杂环正电子发射断层扫描放射性配体的铜介导的 18F-氟化
摘要:用氟 18 (18F) 标记的分子用于正电子发射断层扫描,以可视化,表征和测量体内的生物过程.尽管最近在将 18F 掺入芳烃方面取得了进展,但开发通用且有效的方法来标记药物发现计划所需的放射性配体仍然是一项重大任务.这个完整的描述描述了杂环正电子发射断层扫描 (Pet) 放射性配体的放射合成方法,使用铜介导的 18F 氟化芳基硼试剂与 18F 氟化物作为模型反应.该方法基于一项研究,该研究检查了药物开发中常用的杂环的存在如何影响代表性芳基硼试剂的 18F-氟化效率,以及超过 50 种(杂)芳基硼酸酯的标记.这组数据允许将这种去风险策略应用于七种结构复杂的药物相关含杂环分子的成功放射合成.
DOI:10.1021/jacs.7B03131

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-9012648-B2
优先权日:2012-08-21
标题 :Haptens of risperidone and paliperidone
发明人：HASPESLAGH PIETER RIK; VLIEGEN MAARTEN; HRYHORENKO ERIC; DECORY THOMAS R; SANKARAN BANUMATHI
权利人:JANSSEN PHARMACEUTICA NV; ORTHO CLINICAL DIAGNOSTICS INC
摘要:The invention relates to compounds of Formula I, wherein R1 and R2 are defined in the specification, useful for the synthesis of novel conjugates and immunogens derived from risperidone and paliperidone. The invention also relates to conjugates of a risperidone or paliperidone hapten and a protein.

专利号:US-6897308-B1
优先权日:2000-05-05
标 题 :Process for the preparation of anti-psychotic 3-[2-[-4-(6-fluoro-1,2-benziosoxazol-3-yl)-1-piperidinyl] ethyl]-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one
发明人：VENKATASUBRAMANIAN RADHAKRISHN; GOVIND SATHE DHANANJAY; VASANTRAO SURYAVANSHI CHANDRAK
权利人:RPG LIFE SCIENCES LTD
摘要:A process for the preparation of 3-substituted ethyl-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2,-a]pyrimidin-4-one of the formula IIB: n n nwhere X may be halo, acyloxy, or sulfonyloxy such as tosyloxy or mesyloxy, an intermediate in the synthesis of the anti-psychotic risperidone. The process comprises hydrogenation of 3-substituted ethyl-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one in aqueous inorganic acid medium at atmospheric to 60 psi at 0-100° C. in the presence of a metal catalyst and the product is isolated. A process for the preparation of risperidone of the formula I: n n ncomprising condensation of 3-substituted ethyl-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2,-a]pyrimidin-4-one with 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole in water in the presence of an inorganic base at 25-100° C. and the product is isolated.

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

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

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