CAS: 84163-77-9; 6-Fluoro-3-(4-Piperidinyl)-1,2-Benzisoxazole

相似化合物

84163-13-3 84163-13-3 84163-22-4

上下游产品

CAS号135634-18-3 (2,4-二氟苯基)-(4-哌... | CAS号84162-86-7 1-(2',4'-二氟苯甲酰基... | CAS号84163-13-3 6-氟-3-(4-哌啶基) -... | CAS号84162-80-1 4-(2,4-DIFLUORO... | CAS号498-94-2 4-哌啶甲酸 | CAS号84163-42-8 1-醛基哌啶-4-甲酸 | CAS号84163-43-9 1-甲酰基-哌啶-4-羰酰氯 | CAS号84163-41-7 6-fluoro-3-(1-f... | CAS号84162-94-7 1-formyl-4-(2,4... | CAS号59084-16-1 N-乙酰基哌啶-4-酰氯 | CAS号1189516-65-1 帕潘立酮棕榈酸酯氧化杂质 | CAS号144598-75-4 9－羟基利培酮 | CAS号133454-47-4 伊潘立酮 | CAS号130049-85-3 (R)-9-Hydroxy R... | CAS号106266-06-2 利培酮

1,3-二氟苯置于盐酸,Aluminum (Iii) Chloride,盐酸羟胺,Potassium Hydroxide体系中,用 乙醇,二氯甲烷,水 作为反应溶剂,化学反应 13.0H,反应生成 6-氟-3-(哌啶-4-基)苯并[d]异恶唑
参考文献:一种6-氟-3-(4-哌啶基)-1,2-苯并异噁唑盐酸盐的纯化方法
标题:一种6-氟-3-(4-哌啶基)-1,2-苯并异噁唑盐酸盐的纯化方法
摘要:本发明公开一种利培酮中间体如式ii所示的6‑氟‑3‑(4‑哌啶基)‑1,2‑苯并异噁唑盐酸盐的纯化方法,其特征在于,所述的纯化方法是将6‑氟‑3‑(4‑哌啶基)‑1,2‑苯并异噁唑盐酸盐加入到乙醇中,再加入一定量的水,加热回流至溶清,降温至一定温度进行养晶,然后再降温至‑5~10°C,过滤,烘干得到.本发明提供的6‑氟‑3‑(4‑哌啶基)‑1,2‑苯并异噁唑盐酸盐的纯化方法,能有效地将式ⅴ二聚体分离出去,纯化收率在85%以上,成品的化学纯度可达到99.9%以上,并且在大生产中不会产生放大效应,工艺稳定.

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-2013261308-A1
优先权日:2012-03-29
标题 :One-pot process for the synthesis of iloperidone
发明人：BETTONI PIERGIORGIO; ROLETTO JACOPO; PAISSONI PAOLO
权利人:PROCOS SPA
摘要:Disclosed is a process for the synthesis of iloperidone starting from 4-hydroxy-3-methoxy acetophenone (acetovanillone), 1-chloro-3-bromo propane and 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride, using a one-pot method. n n n n n n n n n n Said process is performed without any intermediate isolation, and is particularly advantageous from the environmental standpoint and in terms of yields, productivity and the purity of the product obtained, both in the reaction mixture and in the crystal isolated.

专利号:EP-2454256-B1
优先权日:2009-07-13
标题 :Process for the synthesis of paliperidone
发明人：RUZIC MILOS; PECAVAR ANICA; PRUDIC DARJA; PLAPER IGOR; KLOBCAR ANDREJ; PLEVNIK MIHA; HVALA JERNEJ
权利人:KRKA D D NOVO MESTO
摘要:The invention describes an improved process for the synthesis and purification of paliperidone.

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.