GR1004073B - Μεθοδος παρασκευης της σιταλοπραμης - Google Patents
Μεθοδος παρασκευης της σιταλοπραμηςInfo
- Publication number
- GR1004073B GR1004073B GR20010100098A GR2001100098A GR1004073B GR 1004073 B GR1004073 B GR 1004073B GR 20010100098 A GR20010100098 A GR 20010100098A GR 2001100098 A GR2001100098 A GR 2001100098A GR 1004073 B GR1004073 B GR 1004073B
- Authority
- GR
- Greece
- Prior art keywords
- group
- compound
- formula
- citalopram
- alkynyl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D307/87—Benzo [c] furans; Hydrogenated benzo [c] furans
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
- A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Steroid Compounds (AREA)
Abstract
παρούσα εφεύρεση αναφέρεται σε μια μέθοδο για την παρασκευή σιταλοπράμης περιλαμβάνουσα την αντίδραση μιάς ενώσεως τύπου (Ι) με μία ένωση έχουσα τον τύπο (ΙΙ) στον οποίο το Χ είναι μια κατάλληλη αποχωριζόμενη ομάδα και το R είναι -CH2-O-Pg, -CH2-NPg1Pg2, -CH2-NMePg1, -CO-N(CH3)2, -CH(OR1)(OR2), -C(OR4)(OR5)(OR6), -COOR3, -CH2-CO-NH2, -CH=CHR7 ή -CO-NHR8 όπου το Pg είναι μία προστατευτική ομάδα μίας ομάδος αλκοόλης, τα Pg1 και Pg2 είναι προστατευτικές ομάδες μίας αμινομάδος, τα R1 και R2 επιλέγονται ανεξάρτητα απο αλκύλιο, αλκενύλιο, αλκυνύλιο και αρύλιο ή αραλκύλιο προαιρετικά υποκατασταθέν με αλκύλιο ή τα R1 και R2 σχηματίζουν ομού μία άλυσο με 2 έως 4 άτομα άνθρακα, τα R3, R4, R5, R6 και R7 επιλέγονται ανεξάρτητα απο αλκύλιο, αλκενύλιο, αλκυνύλιο και αρύλιο ή αραλκύλιο προαιρετικά υποκατασταθέν με αλκύλιο και το R8 είναι υδρογόνο ή μεθύλιο για το σχηματισμό μίας ενώσεως τύπου (ΙΙΙ) στον οποίο το R είναι όπως ορίσθηκε ανωτέρω ακολουθούμενη απο την μετατροπή της ομάδος R σε μία ομάδα διμεθυλαμινομεθυλίου και την απομόνωση της σιταλοπράμης υπό την μορφή βάσεως ή φαρμακευτικά αποδεκτού αλατός της.
ΰ
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA200000296 | 2000-02-24 | ||
| DKPA200000401 | 2000-03-13 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| GR20010100098A GR20010100098A (el) | 2001-10-31 |
| GR1004073B true GR1004073B (el) | 2002-11-26 |
Family
ID=26068779
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| GR20010100098A GR1004073B (el) | 2000-02-24 | 2001-02-22 | Μεθοδος παρασκευης της σιταλοπραμης |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US6420574B2 (el) |
| EP (1) | EP1259501A2 (el) |
| JP (1) | JP2003523955A (el) |
| KR (1) | KR20020081355A (el) |
| CN (1) | CN1608057A (el) |
| AR (1) | AR029658A1 (el) |
| AU (1) | AU2001235358A1 (el) |
| BE (1) | BE1011177A6 (el) |
| BG (1) | BG107061A (el) |
| BR (1) | BR0108937A (el) |
| CA (1) | CA2401236A1 (el) |
| EA (1) | EA005315B1 (el) |
| FR (1) | FR2805812A1 (el) |
| GR (1) | GR1004073B (el) |
| HR (1) | HRP20020660A2 (el) |
| HU (1) | HUP0300212A2 (el) |
| IE (1) | IES20010163A2 (el) |
| IL (1) | IL151059A0 (el) |
| IS (1) | IS6487A (el) |
| IT (1) | ITMI20010386A1 (el) |
| MX (1) | MXPA02008228A (el) |
| NL (1) | NL1017415C1 (el) |
| NO (1) | NO20023928L (el) |
| PL (1) | PL363119A1 (el) |
| SK (1) | SK13672002A3 (el) |
| WO (1) | WO2001043525A2 (el) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR022329A1 (es) | 1999-01-29 | 2002-09-04 | Lundbeck & Co As H | Metodo para la preparacion de 5-cianoftalida |
| ATE237604T1 (de) * | 1999-04-14 | 2003-05-15 | Lundbeck & Co As H | Verfahren zur herstellung von citalopram |
| ITMI991581A1 (it) * | 1999-06-25 | 2001-01-15 | Lundbeck & Co As H | Metodo per la preparazione di citalopram |
| HUP0200169A3 (en) | 1999-10-25 | 2002-11-28 | Lundbeck & Co As H | Method for the preparation of citalopram |
| AR026063A1 (es) | 1999-11-01 | 2002-12-26 | Lundbeck & Co As H | Metodo para la preparacion de 5-carboxiftalida. |
| US6310222B1 (en) | 1999-11-01 | 2001-10-30 | Sumika Fine Chemicals Co., Ltd. | Production method of 5-phthalancarbonitrile compound, intermediate therefor and production method of the intermediate |
| WO2001047909A1 (en) | 1999-12-28 | 2001-07-05 | H. Lundbeck A/S | Method for the preparation of citalopram |
| PL198803B1 (pl) | 1999-12-30 | 2008-07-31 | Lundbeck & Co As H | Sposób wytwarzania 5-cyjano-3H-izobenzofuran-1-onu |
| ES2206177T3 (es) * | 2000-01-14 | 2004-05-16 | H. Lundbeck A/S | Metodo para la preparacion de 5-cianoftalida. |
| US6433196B1 (en) * | 2000-02-17 | 2002-08-13 | Sumika Fine Chemicals Co., Ltd. | Production method of citalopram, intermediate therefor and production method of the intermediate |
| IES20010157A2 (en) * | 2000-03-03 | 2002-03-06 | Lundbeck & Co As H | Method for the preparation of citalopram |
| IES20010206A2 (en) | 2000-03-13 | 2002-03-06 | Lundbeck & Co As H | Method for the preparation of citalopram |
| BR0109176A (pt) | 2000-03-13 | 2003-04-22 | Lundbeck & Co As H | Método para preparação de citalopram e composto da fórmula |
| CA2402553A1 (en) * | 2000-03-13 | 2001-09-20 | H. Lundbeck A/S | Stepwise alkylation of 5-substituted 1-(4-fluorophenyl)-1,3-dihydroisobenzofurans |
| IL151488A0 (en) | 2000-03-14 | 2003-04-10 | Lundbeck & Co As H | Method for the preparation of citalopram |
| EP1274699A1 (en) * | 2000-03-16 | 2003-01-15 | H. Lundbeck A/S | Method for the preparation of 5-cyano-1-(4-fluorophenyl)-1,3-dihydroisobenzofurans |
| AR032455A1 (es) | 2000-05-12 | 2003-11-12 | Lundbeck & Co As H | Metodo para la preparacion de citalopram, un intermediario empleado en el metodo, un metodo para la preparacion del intermediario empleado en el metodo y composicion farmaceutica antidepresiva |
| CA2354880C (en) | 2000-08-18 | 2003-06-03 | H. Lundbeck A/S | Method for the preparation of citalopram |
| IL147226A (en) | 2000-12-22 | 2006-04-10 | Lundbeck & Co As H | Process for the preparation of pure cithalopram |
| AR034759A1 (es) * | 2001-07-13 | 2004-03-17 | Lundbeck & Co As H | Metodo para la preparacion de escitalopram |
| MXPA04004368A (es) * | 2001-11-08 | 2004-08-11 | Sepracor Inc | Metodos para tratar depresion y otros transtornos del sistema nervioso central utilizando desmetil-y didesmetil-metabolitos del citalopram enantiomericamente enriquecidos. |
| PE20040991A1 (es) | 2002-08-12 | 2004-12-27 | Lundbeck & Co As H | Separacion de intermediarios para la preparacion de escitalopram |
| US20050154052A1 (en) * | 2003-03-24 | 2005-07-14 | Hetero Drugs Limited | Novel crystalline forms of (s)-citalopram oxalate |
| WO2005047274A1 (en) * | 2003-11-12 | 2005-05-26 | Dr. Reddy's Laboratories, Inc. | Preparation of escitalopram |
| TWI339651B (en) | 2004-02-12 | 2011-04-01 | Lundbeck & Co As H | Method for the separation of intermediates which may be used for the preparation of escitalopram |
| GB0601286D0 (en) | 2006-01-23 | 2006-03-01 | Sandoz Ag | Asymmetric synthesis |
| AU2008252631B2 (en) * | 2007-05-18 | 2012-12-20 | Cipla Limited | Process for the preparation of escitalopram via desmethylcitalopram, optical resolution and methylation of the S-isomer |
| US9339500B2 (en) * | 2008-03-04 | 2016-05-17 | Intra-Cellular Therapies, Inc. | Methods of treating vasomotor symptoms |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1143702A (el) | 1965-03-18 | |||
| GB1526331A (en) * | 1976-01-14 | 1978-09-27 | Kefalas As | Phthalanes |
| GB8419963D0 (en) | 1984-08-06 | 1984-09-12 | Lundbeck & Co As H | Intermediate compound and method |
| US5296007A (en) | 1986-11-17 | 1994-03-22 | Ensci Inc. | Process for removing sulfur from coal |
| GB8814057D0 (en) | 1988-06-14 | 1988-07-20 | Lundbeck & Co As H | New enantiomers & their isolation |
| DE19626659A1 (de) | 1996-07-03 | 1998-01-08 | Basf Ag | Verfahren zur Herstellung von Phthaliden |
| DE19627697A1 (de) | 1996-07-10 | 1998-01-15 | Basf Ag | Verfahren zur Herstellung von Phthaliden |
| JP3526581B2 (ja) | 1997-07-08 | 2004-05-17 | ハー・ルンドベック・アクティーゼルスカブ | シタロプラムの製造方法 |
| UA62985C2 (en) | 1997-11-10 | 2004-01-15 | Lunnbeck As H | A method for the preparation of citalopram |
| CZ292911B6 (cs) | 1997-11-11 | 2004-01-14 | H. Lundbeck A/S | Způsob výroby citalopramu |
| PL199423B1 (pl) | 1998-10-20 | 2008-09-30 | Lundbeck & Co As H | Sposób wytwarzania citalopramu |
| TR200101796T2 (tr) | 1998-12-23 | 2001-11-21 | H. Lundbeck A/S | 5-Siyanofitalitin preparasyonuna yönelik metot |
| AR022329A1 (es) | 1999-01-29 | 2002-09-04 | Lundbeck & Co As H | Metodo para la preparacion de 5-cianoftalida |
| ATE237604T1 (de) | 1999-04-14 | 2003-05-15 | Lundbeck & Co As H | Verfahren zur herstellung von citalopram |
| ITMI991579A1 (it) | 1999-06-25 | 2001-01-15 | Lundbeck & Co As H | Metodo per la preparazione di citalopram |
| ITMI991581A1 (it) | 1999-06-25 | 2001-01-15 | Lundbeck & Co As H | Metodo per la preparazione di citalopram |
| GB2360281B (en) | 1999-10-25 | 2002-01-16 | Lundbeck & Co As H | Method for the preparation of citalopram |
| US6310222B1 (en) | 1999-11-01 | 2001-10-30 | Sumika Fine Chemicals Co., Ltd. | Production method of 5-phthalancarbonitrile compound, intermediate therefor and production method of the intermediate |
-
2001
- 2001-02-21 NL NL1017415A patent/NL1017415C1/nl not_active IP Right Cessation
- 2001-02-21 FR FR0102339A patent/FR2805812A1/fr active Pending
- 2001-02-22 EA EA200200898A patent/EA005315B1/ru not_active IP Right Cessation
- 2001-02-22 BR BR0108937-4A patent/BR0108937A/pt not_active IP Right Cessation
- 2001-02-22 CN CNA018055567A patent/CN1608057A/zh active Pending
- 2001-02-22 CA CA002401236A patent/CA2401236A1/en not_active Abandoned
- 2001-02-22 MX MXPA02008228A patent/MXPA02008228A/es unknown
- 2001-02-22 WO PCT/DK2001/000123 patent/WO2001043525A2/en not_active Application Discontinuation
- 2001-02-22 KR KR1020027011111A patent/KR20020081355A/ko not_active Application Discontinuation
- 2001-02-22 PL PL01363119A patent/PL363119A1/xx not_active Application Discontinuation
- 2001-02-22 EP EP01907389A patent/EP1259501A2/en not_active Withdrawn
- 2001-02-22 GR GR20010100098A patent/GR1004073B/el unknown
- 2001-02-22 JP JP2001544478A patent/JP2003523955A/ja not_active Withdrawn
- 2001-02-22 IL IL15105901A patent/IL151059A0/xx unknown
- 2001-02-22 AU AU2001235358A patent/AU2001235358A1/en not_active Abandoned
- 2001-02-22 HU HU0300212A patent/HUP0300212A2/hu unknown
- 2001-02-22 IE IE20010163A patent/IES20010163A2/en not_active IP Right Cessation
- 2001-02-22 SK SK1367-2002A patent/SK13672002A3/sk not_active Application Discontinuation
- 2001-02-23 AR ARP010100836A patent/AR029658A1/es not_active Application Discontinuation
- 2001-02-23 BE BE2001/0126A patent/BE1011177A6/fr not_active IP Right Cessation
- 2001-02-26 IT IT2001MI000386A patent/ITMI20010386A1/it unknown
- 2001-02-26 US US09/794,762 patent/US6420574B2/en not_active Expired - Lifetime
-
2002
- 2002-07-29 IS IS6487A patent/IS6487A/is unknown
- 2002-08-09 HR HRP20020660 patent/HRP20020660A2/hr not_active Application Discontinuation
- 2002-08-19 NO NO20023928A patent/NO20023928L/no not_active Application Discontinuation
- 2002-09-04 BG BG107061A patent/BG107061A/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| IL151059A0 (en) | 2003-04-10 |
| IES20010163A2 (en) | 2002-03-06 |
| WO2001043525A3 (en) | 2002-01-31 |
| HRP20020660A2 (en) | 2004-12-31 |
| AU2001235358A1 (en) | 2001-06-25 |
| US20010027256A1 (en) | 2001-10-04 |
| FR2805812A1 (fr) | 2001-09-07 |
| IS6487A (is) | 2002-07-29 |
| NO20023928D0 (no) | 2002-08-19 |
| SK13672002A3 (sk) | 2003-03-04 |
| US6420574B2 (en) | 2002-07-16 |
| AR029658A1 (es) | 2003-07-10 |
| EA005315B1 (ru) | 2004-12-30 |
| HUP0300212A2 (hu) | 2003-06-28 |
| NO20023928L (no) | 2002-08-19 |
| WO2001043525A2 (en) | 2001-06-21 |
| CN1608057A (zh) | 2005-04-20 |
| BR0108937A (pt) | 2003-06-17 |
| ITMI20010386A1 (it) | 2002-08-26 |
| BG107061A (en) | 2003-05-30 |
| MXPA02008228A (es) | 2004-04-05 |
| EP1259501A2 (en) | 2002-11-27 |
| PL363119A1 (en) | 2004-11-15 |
| JP2003523955A (ja) | 2003-08-12 |
| BE1011177A6 (fr) | 2001-07-03 |
| NL1017415C1 (nl) | 2001-05-18 |
| EA200200898A1 (ru) | 2003-02-27 |
| GR20010100098A (el) | 2001-10-31 |
| KR20020081355A (ko) | 2002-10-26 |
| CA2401236A1 (en) | 2001-06-21 |
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