CAS: 41078-70-0; 3-(2-Chloroethyl)-2-Methyl-4H-Pyrido[1,2-A]Pyrimidin-4-One

相似化合物

260273-82-3 58837-31-3 260273-81-2

上下游产品

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63234-80-0 3-(2-氯乙基)-2-甲基-... | CAS号75444-65-4 3-(2-(4-(4-氟苯甲酰...

α-乙酰基-γ-丁内酯置于对甲苯磺酸,三氯氧磷体系中,用 甲苯 作为反应溶剂,化学反应 13.0H,反应生成 3-(2-氯乙基)-2-甲基吡啶并[1,2-A]嘧啶-4-酮
参考文献:Synthesis Of 3-(2-Chloroethyl)-2-Methyl-6,7,8,9-Tetrahydro-4H-Pyrido[1,2-A] Pyrimidin-4-One Derivatives As Antibacterial Agents
标题:Synthesis Of 3-(2-Chloroethyl)-2-Methyl-6,7,8,9-Tetrahydro-4H-Pyrido[1,2-A] Pyrimidin-4-One Derivatives As Antibacterial Agents
摘要:一系列新颖的3-(2-氯乙基)-2-甲基-6,7,8,9-四氢-4H-吡啶[1,2-A]嘧啶-4-酮的脂肪族/芳香族/杂环胺衍生物以非常好产率合成.合成的化合物通过¹h-NMR,Ftir和元素分析进行了表征.所有合成的化合物通过琼脂孔扩散法和微稀释法 Screened 了其对标准抗菌株的体外抗菌活性,包括革兰氏阳性菌(枯草芽孢杆菌 Mtcc 121 和表皮葡萄球菌 435)以及革兰氏阴性菌(盲肠黄单胞菌 7903 和铜绿假单胞菌 Mtcc 7908).带有取代杂环哌嗪基团的化合物显示出了非常好的活性.特别是化合物 6I 的活性相较于标准药物链霉素硫酸盐提高了两倍.
DOI:10.2174/1573406411309020008

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-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

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