AR069621A1 - Sintesis de paliperidona - Google Patents

Sintesis de paliperidona

Info

Publication number
AR069621A1
AR069621A1 ARP080105347A ARP080105347A AR069621A1 AR 069621 A1 AR069621 A1 AR 069621A1 AR P080105347 A ARP080105347 A AR P080105347A AR P080105347 A ARP080105347 A AR P080105347A AR 069621 A1 AR069621 A1 AR 069621A1
Authority
AR
Argentina
Prior art keywords
formula
compound
group
leaving group
defined above
Prior art date
Application number
ARP080105347A
Other languages
English (en)
Inventor
Jozef Krajcovic
Barti Jiri
Petr Benovsky
Original Assignee
Synthon Bv
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Synthon Bv filed Critical Synthon Bv
Publication of AR069621A1 publication Critical patent/AR069621A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Compuesto intermediario de formula (6) y su uso para preparar paliperidona. Reivindicacion 1: Un proceso caracterizado porque comprende: a) acilar bajo condiciones Vilsmeier-Haack o Friedel-Crafts un compuesto de la formula (5): en donde, G se selecciona del grupo que consiste de (i) un grupo saliente tal como halo, por ejemplo, cloro, bromo o iodo; o sulfoniloxi, por ejemplo, metansulfoniloxi, trifluorometansulfoniloxi, bencensulfoniloxi, 4-metilbencensulfoniloxi, o 4-metoxibencensulfoniloxi; (ii) un grupo de la formula (4): en donde, L representa un grupo saliente reactivo; y (iii) un grupo de la formula (3) para formar un compuesto de la formula (6), en donde, R' representa hidrogeno o un grupo alquilo C1-19 y G es como se define con anterioridad; y b) transformar dicho compuesto de la formula (6) con un peroxo-compuesto para formar un compuesto de la formula (1): en donde, R es hidrogeno o grupo acilo C1-20 y G es como se define con anterioridad, y preferentemente G representa dicho grupo saliente, preferentemente cloro.
ARP080105347A 2007-12-10 2008-12-10 Sintesis de paliperidona AR069621A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US1254607P 2007-12-10 2007-12-10

Publications (1)

Publication Number Publication Date
AR069621A1 true AR069621A1 (es) 2010-02-03

Family

ID=40352126

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP080105347A AR069621A1 (es) 2007-12-10 2008-12-10 Sintesis de paliperidona

Country Status (6)

Country Link
US (1) US7977480B2 (es)
EP (1) EP2235009B1 (es)
AR (1) AR069621A1 (es)
CL (1) CL2008003667A1 (es)
ES (1) ES2436658T3 (es)
WO (1) WO2009074333A1 (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR069637A1 (es) 2007-12-10 2010-02-10 Novartis Ag Derivados de pirazinas
US7932385B2 (en) * 2008-07-11 2011-04-26 Synthon Bv Paliperidone ketone
WO2010003702A1 (en) * 2008-07-11 2010-01-14 Synthon B.V. Synthesis of paliperidone
KR101867988B1 (ko) * 2016-11-02 2018-06-15 주식회사 엔지켐생명과학 팔리페리돈 중간체 및 이를 이용한 팔리페리돈의 제조방법
CN117777131B (zh) * 2024-02-27 2024-06-11 合肥华方医药科技有限公司 一种帕利哌酮及其关键中间体的合成方法

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4804663A (en) 1985-03-27 1989-02-14 Janssen Pharmaceutica N.V. 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles
CA2000786C (en) * 1988-11-07 1999-01-26 Cornelus G. M. Janssen 3-piperidinyl-1,2-benzisoxazoles
US5158952A (en) 1988-11-07 1992-10-27 Janssen Pharmaceutica N.V. 3-[2-[4-(6-fluoro-1,2-benzisoxozol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9 tetrahydro-9-hydroxy-2-methyl-4H-pyrido [1,2-a]pyrimidin-4-one, compositions and method of use
RU2126406C1 (ru) 1993-11-23 1999-02-20 Жансен Фармасетика Н.В. Эфирные производные 9-гидрокси-пиридо[1,2-а]пиримидин-4-она, способ их получения, композиция, обладающая антипсихотической активностью и способ ее получения
CN101484437A (zh) 2005-05-04 2009-07-15 V.B.医疗保险私人有限公司 从双(三氯甲基)碳酸酯合成用于氯化反应的Vilsmeier-Haack试剂
EP2178872A1 (en) 2007-07-27 2010-04-28 Synthon B.V. Paliperidone derivatives

Also Published As

Publication number Publication date
WO2009074333A1 (en) 2009-06-18
US20090156810A1 (en) 2009-06-18
EP2235009A1 (en) 2010-10-06
CL2008003667A1 (es) 2010-06-04
US7977480B2 (en) 2011-07-12
EP2235009B1 (en) 2013-10-30
ES2436658T3 (es) 2014-01-03

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