CY1119991T1 - Μεθοδος για την παραγωγη 2-[4-(3- ή 2-φθοροβενζυλοξυ)βενζυλαμινο]προπαναμιδιων με υψηλο βαθμο καθαροτητας - Google Patents
Μεθοδος για την παραγωγη 2-[4-(3- ή 2-φθοροβενζυλοξυ)βενζυλαμινο]προπαναμιδιων με υψηλο βαθμο καθαροτηταςInfo
- Publication number
- CY1119991T1 CY1119991T1 CY20181100007T CY181100007T CY1119991T1 CY 1119991 T1 CY1119991 T1 CY 1119991T1 CY 20181100007 T CY20181100007 T CY 20181100007T CY 181100007 T CY181100007 T CY 181100007T CY 1119991 T1 CY1119991 T1 CY 1119991T1
- Authority
- CY
- Cyprus
- Prior art keywords
- propanamides
- fluorobenzyloxy
- reaction
- benzylamine
- procedure
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 3
- QLNJFJADRCOGBJ-UHFFFAOYSA-N propionamide Chemical class CCC(N)=O QLNJFJADRCOGBJ-UHFFFAOYSA-N 0.000 title abstract 3
- -1 2-fluorobenzyloxy Chemical group 0.000 title abstract 2
- WGQKYBSKWIADBV-UHFFFAOYSA-N benzylamine Chemical compound NCC1=CC=CC=C1 WGQKYBSKWIADBV-UHFFFAOYSA-N 0.000 title 2
- 239000002262 Schiff base Substances 0.000 abstract 2
- 150000004753 Schiff bases Chemical class 0.000 abstract 2
- 239000003960 organic solvent Substances 0.000 abstract 2
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 150000007513 acids Chemical class 0.000 abstract 1
- 239000002585 base Substances 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000000440 benzylamino group Chemical group [H]N(*)C([H])([H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 239000003638 chemical reducing agent Substances 0.000 abstract 1
- 239000012535 impurity Substances 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 229910052700 potassium Inorganic materials 0.000 abstract 1
- 239000011591 potassium Substances 0.000 abstract 1
- 238000011946 reduction process Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 239000000725 suspension Substances 0.000 abstract 1
Classifications
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C251/00—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
- C07C251/02—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton containing imino groups
- C07C251/24—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton containing imino groups having carbon atoms of imino groups bound to carbon atoms of six-membered aromatic rings
-
- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
-
- A—HUMAN NECESSITIES
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- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- C07C231/00—Preparation of carboxylic acid amides
- C07C231/12—Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C231/00—Preparation of carboxylic acid amides
- C07C231/22—Separation; Purification; Stabilisation; Use of additives
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- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
Μία μέθοδος για τη λήψη θεραπευτικά δραστικών 2-[4-(3- και 2-(φθοροβενζυλοξυ)βενζυλαμινο]προπαναμιδίων και των αλάτων αυτών με φαρμακευτικά αποδεκτά οξέα με υψηλό βαθμό καθαρότητας, συγκεκριμένα με μία περιεκτικότητα ακαθαρσιών διβενζυλικών παραγώγων χαμηλότερη από 0.03 %, κατά προτίμηση χαμηλότερη από 0.01 % κατά βάρος. Η μέθοδος διεξάγεται δια υποβολής των ενδιαμέσων ενώσεων βάσεων Schiff 2-[4-(3- και 2-φθοροβενζυλοξυ)βενζυλιδεναμινο]προπαναμιδίων σε μία αντίδραση αναγωγής, με έναν αναγωγικό παράγοντα που επιλέγεται από βοροϋδρίδιο του νατρίου και βοροϋδρίδιο του καλίου σε μία κατάλληλη ποσότητα ενός οργανικού διαλύτη που επιλέγεται από C1-C5 κατώτερες αλκανόλες, επιτρέποντας τον σχηματισμό και την παρουσία κατά τη διάρκεια ενός σημαντικού μέρους της πορείας της αντίδρασης αναγωγής ενός εναιωρήματος της βάσης Schiff εντός του κεκορεσμένου διαλύματος της βάσης Schiff εντός του ίδιου οργανικού διαλύτη.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07023937 | 2007-12-11 | ||
| PCT/EP2008/066559 WO2009074478A1 (en) | 2007-12-11 | 2008-12-01 | Process for the production of 2-[4-(3- or 2-fluorobenzyloxy)benzylamino]propanamides with high purity degree |
| EP08860373.3A EP2229351B1 (en) | 2007-12-11 | 2008-12-01 | Process for the production of 2-[4-(3- or 2-fluorobenzyloxy)benzylamino]propanamides with high purity degree |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CY1119991T1 true CY1119991T1 (el) | 2018-12-12 |
Family
ID=39301684
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CY20181100007T CY1119991T1 (el) | 2007-12-11 | 2018-01-03 | Μεθοδος για την παραγωγη 2-[4-(3- ή 2-φθοροβενζυλοξυ)βενζυλαμινο]προπαναμιδιων με υψηλο βαθμο καθαροτητας |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US8530701B2 (el) |
| EP (2) | EP2229351B1 (el) |
| JP (2) | JP5460613B2 (el) |
| KR (2) | KR101709498B1 (el) |
| CN (2) | CN104523668B (el) |
| AR (1) | AR071267A1 (el) |
| AU (1) | AU2008334778B2 (el) |
| BR (1) | BRPI0820657A2 (el) |
| CA (2) | CA2936209C (el) |
| CY (1) | CY1119991T1 (el) |
| DK (1) | DK2229351T3 (el) |
| EA (2) | EA019898B1 (el) |
| ES (2) | ES2837000T3 (el) |
| HK (2) | HK1145673A1 (el) |
| HR (1) | HRP20180210T1 (el) |
| HU (1) | HUE036232T2 (el) |
| IL (1) | IL205872A (el) |
| LT (1) | LT2229351T (el) |
| MX (1) | MX2010006278A (el) |
| NO (1) | NO2229351T3 (el) |
| NZ (1) | NZ585806A (el) |
| PL (1) | PL2229351T3 (el) |
| PT (1) | PT2229351T (el) |
| RS (1) | RS56803B1 (el) |
| SI (1) | SI2229351T1 (el) |
| TW (1) | TWI429425B (el) |
| WO (1) | WO2009074478A1 (el) |
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| SI1658062T1 (sl) * | 2003-08-25 | 2010-05-31 | Newron Pharm Spa | Alfa aminoamidni derivati uporabni kot protivnetna sredstva |
| ES2602069T3 (es) * | 2006-06-19 | 2017-02-17 | Newron Pharmaceuticals S.P.A. | 2-[4-(3- y 2-fluorobenciloxi)bencilamino]propanamidas de grado de pureza elevado para la utilización como medicamentos y formulaciones farmacéuticas que las contienen |
| RS56803B1 (sr) * | 2007-12-11 | 2018-04-30 | Newron Pharm Spa | Postupak za proizvodnju 2-[4-(3-ili2-fluorobenziloksi)benzilamino] propanamida sa visokim stepenom čistoće |
| EP2314569A1 (en) * | 2009-10-22 | 2011-04-27 | Merck Patent GmbH | Novel polymorphic forms of (S)-2-[4-(3-Fluoro-benzyloxy)-benzylamino]-propionamide mesylate salt and processes of manufacturing thereof |
| EP2563355B1 (en) * | 2010-04-27 | 2016-06-08 | Newron Pharmaceuticals S.p.A. | Process for the production of ralfinamide methanesulfonate salts or their R-enantiomers |
| MX2013005242A (es) | 2010-11-11 | 2013-06-12 | Redx Pharma Ltd | Derivados de farmacos. |
| CN103044279B (zh) * | 2012-12-21 | 2015-07-08 | 苏州永健生物医药有限公司 | 一种n-香豆酰多巴胺的合成方法 |
| KR101705718B1 (ko) * | 2013-12-30 | 2017-02-14 | 이화여자대학교 산학협력단 | 신규한 아미드 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 포함하는 통증의 예방 또는 치료용 약학적 조성물 |
| CN104292128A (zh) * | 2014-07-01 | 2015-01-21 | 南京正科制药有限公司 | 一种沙芬酰胺晶型a |
| CN105017060B (zh) * | 2015-07-03 | 2017-06-16 | 南京正大天晴制药有限公司 | 一种沙芬酰胺新晶型及其制备方法 |
| CN113072436A (zh) * | 2015-07-24 | 2021-07-06 | 上海医药集团股份有限公司 | 一种苄基芳基醚的制备方法 |
| CN105061245A (zh) * | 2015-08-25 | 2015-11-18 | 成都维恒医药科技有限公司 | 一种高纯度沙芬酰胺的制备方法 |
| CN106349269B (zh) * | 2016-08-24 | 2018-08-31 | 浙江美诺华药物化学有限公司 | 2-(3-氟苄氧基)-5-甲酰基苯硼酸及其制备方法 |
| CN106565521B (zh) * | 2016-08-24 | 2019-03-08 | 浙江美诺华药物化学有限公司 | (s)-2-[3-(3-氟苄基)-4-(3-氟苄氧基)苄氨基]丙酰胺及其盐的制备方法 |
| CN106565442B (zh) * | 2016-08-24 | 2019-07-16 | 浙江美诺华药物化学有限公司 | 3-(3-氟苄基)-4-(3-氟苄氧基)苯甲醛的制备方法 |
| CN106632223B (zh) * | 2016-08-24 | 2019-04-23 | 浙江美诺华药物化学有限公司 | 2-(3-溴-4-(3-氟苄氧基)苯基)-1,3-二氧戊环及其制备方法 |
| CN106596828B (zh) * | 2016-12-15 | 2018-09-25 | 扬子江药业集团有限公司 | 一种甲磺酸沙芬酰胺有关物质的检测方法 |
| WO2019167085A1 (en) * | 2018-03-01 | 2019-09-06 | Msn Laboratories Private Limited, R&D Center | Process for the preparation of (s)-2-[[4-[(3-fluorophenyl)methoxy]phenyl]methyl]amino propanamide methanesulfonate |
| WO2020136671A1 (en) * | 2018-12-27 | 2020-07-02 | Natco Pharma Limited | Improved process for the preparation of lapatinib base and it's anhydrous ditosylate salt |
| EP3725768A1 (en) * | 2019-04-17 | 2020-10-21 | Newron Pharmaceuticals S.p.A. | Process for the production of substituted 2-[2-(phenyl) ethylamino]alkaneamide derivatives |
| US11111208B2 (en) | 2019-06-17 | 2021-09-07 | RK Pharma Solutions LLC | Process for the preparation of safinamide mesylate intermediate |
| ES2977486T3 (es) * | 2019-08-06 | 2024-08-26 | Medichem Sa | Proceso para preparar safinamida |
| CN113444010B (zh) * | 2020-03-28 | 2023-09-05 | 南京正大天晴制药有限公司 | 一种沙芬酰胺有关物质的制备方法 |
| CN112028754A (zh) * | 2020-06-17 | 2020-12-04 | 浙江美诺华药物化学有限公司 | 一种甲磺酸沙芬酰胺中间体的制备方法 |
| CN114088830B (zh) * | 2021-11-10 | 2022-09-23 | 石家庄四药有限公司 | 一种4-(3-氟苄氧基)苯甲醛中异构体的检测方法 |
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| IL94466A (en) * | 1989-05-25 | 1995-01-24 | Erba Carlo Spa | Pharmaceutical preparations containing the history of A-amino carboxamide N-phenylalkyl are converted into such new compounds and their preparation |
| GB9727523D0 (en) | 1997-12-31 | 1998-02-25 | Pharmacia & Upjohn Spa | Alpha-aminoamide derivatives useful as analgesic agents |
| US6335354B2 (en) * | 2000-03-31 | 2002-01-01 | Cocensys Inc. | Aminopyridines and methods of using thereof |
| RU2295337C2 (ru) | 2001-09-03 | 2007-03-20 | Ньюрон Фармасьютикалс Спа | Фармацевтическая композиция, содержащая габапентин или его аналог и альфа-аминоамид, и ее применение в качестве анальгетика |
| EP1438956A1 (en) | 2003-01-16 | 2004-07-21 | Newron Pharmaceuticals S.p.A. | Alpha-aminoamide derivatives useful as antimigraine agents |
| WO2004066987A2 (en) * | 2003-01-30 | 2004-08-12 | Dynogen Pharmaceuticals, Inc. | Use of sodium channel modulators for treating gastrointestinal tract disorders |
| AR044007A1 (es) | 2003-04-11 | 2005-08-24 | Newron Pharmaceuticals Inc | Metodos para el tratamiento de la enfermedad de parkinson |
| TW200507850A (en) | 2003-07-25 | 2005-03-01 | Kyowa Hakko Kogyo Kk | Pharmaceutical composition |
| SI1658062T1 (sl) | 2003-08-25 | 2010-05-31 | Newron Pharm Spa | Alfa aminoamidni derivati uporabni kot protivnetna sredstva |
| EP1557166A1 (en) | 2004-01-21 | 2005-07-27 | Newron Pharmaceuticals S.p.A. | Alpha-aminoamide derivatives useful in the treatment of lower urinary tract disorders |
| EP1588704A1 (en) | 2004-04-22 | 2005-10-26 | Newron Pharmaceuticals S.p.A. | Alpha-aminoamide derivatives useful in the treatment of restless legs syndrome and addictive disorders |
| PT1809271E (pt) | 2004-09-10 | 2010-08-30 | Newron Pharm Spa | Utilização de (halogenobenziloxi)benzilamino-propanamidas para o fabrico de medicamentos activos como moduladores selectivos dos canais de sódio e/ou de cálcio |
| ES2602069T3 (es) * | 2006-06-19 | 2017-02-17 | Newron Pharmaceuticals S.P.A. | 2-[4-(3- y 2-fluorobenciloxi)bencilamino]propanamidas de grado de pureza elevado para la utilización como medicamentos y formulaciones farmacéuticas que las contienen |
| RS56803B1 (sr) * | 2007-12-11 | 2018-04-30 | Newron Pharm Spa | Postupak za proizvodnju 2-[4-(3-ili2-fluorobenziloksi)benzilamino] propanamida sa visokim stepenom čistoće |
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2008
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- 2008-12-01 CN CN201410639898.7A patent/CN104523668B/zh active Active
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