AR069621A1 - Sintesis de paliperidona - Google Patents
Sintesis de paliperidonaInfo
- 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
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.
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)
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)
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 |
-
2008
- 2008-12-10 WO PCT/EP2008/010562 patent/WO2009074333A1/en active Application Filing
- 2008-12-10 AR ARP080105347A patent/AR069621A1/es unknown
- 2008-12-10 EP EP08860056.4A patent/EP2235009B1/en not_active Not-in-force
- 2008-12-10 US US12/331,952 patent/US7977480B2/en not_active Expired - Fee Related
- 2008-12-10 ES ES08860056.4T patent/ES2436658T3/es active Active
- 2008-12-10 CL CL2008003667A patent/CL2008003667A1/es unknown
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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