CAS: 147687-17-0; 9-(Benzyloxy)-3-(2-Chloroethyl)-2-Methyl-4H-Pyrido[1,2-A]Pyrimidin-4-One

上下游产品

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

2-氨基-3-苄氧基吡啶置于对甲苯磺酸,三氯氧磷体系中,用 乙二醇二甲醚,甲苯 用作溶剂,化学反应 6.0H,反应生成3-(2-氯乙基)-2-甲基-9-苄氧基-4H-吡啶并[1,2A]嘧啶-4酮
参考文献:一种高纯度帕利哌酮中间体的制备方法
标题:一种高纯度帕利哌酮中间体的制备方法
摘要:本发明属医药技术领域;具体公开了一种帕利哌酮关键中间体3‑(2‑氯乙基)‑9‑羟基‑2‑甲基‑6,7,8,9‑四氢‑4H‑吡啶并[1,2‑a]嘧啶‑4‑酮的制备方法,具体制备方法为:以2‑氨基‑3‑羟基吡啶为起始原料,经苄基保护,与α‑乙酰基‑γ‑丁内酯关环,氯代制得9‑(苄氧基)‑3‑(2‑氯乙基)‑2‑甲基‑4H‑吡啶并[1,2‑a]嘧啶‑4‑酮;然后将9‑(苄氧基)‑3‑(2‑氯乙基)‑2‑甲基‑4H‑吡啶并[1,2‑a]嘧啶‑4‑酮溶解在醇溶剂中,加入酸和钯炭催化剂,控制氢气压力,反应完全后,经过滤,浓缩,调ph值,萃取,浓缩,精制的工序,得到类白色粉末状的3‑(2‑氯乙基)‑9‑羟基‑2‑甲基‑6,7,8,9‑四氢‑4H‑吡啶并[1,2‑a]嘧啶‑4‑酮;该制备方法周期短,产品颜色类白色,收率达70%以上,纯度达99%以上,没有掉氯副产物的有关杂质,适合工业化放大生产.

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-11667666-B2
优先权日:2020-01-20
标题 :Methods and compositions for treatment of cancer
发明人：SINGHAL ANUJ
权利人:CFD RES CORPORATION
摘要:In an aspect, the disclosure pertains to inhibitors of ANGPTL4; synthesis methods for making disclosed compounds; pharmaceutical compositions comprising disclosed compounds; methods of treating disorders of uncontrolled cellular proliferation, e.g., a cancer; and methods of treating a disease associated with an ANGPTL4 dysfunction using disclosed compounds and pharmaceutical compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

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