AR074151A1 - Un derivado de benzoilbencenoacetamida, proceso de preparacion del mismo, forma polimorfica b de dicho compuesto, proceso de obtencion de dicha forma polimorfica b y su uso - Google Patents
Un derivado de benzoilbencenoacetamida, proceso de preparacion del mismo, forma polimorfica b de dicho compuesto, proceso de obtencion de dicha forma polimorfica b y su usoInfo
- Publication number
- AR074151A1 AR074151A1 ARP090102128A ARP090102128A AR074151A1 AR 074151 A1 AR074151 A1 AR 074151A1 AR P090102128 A ARP090102128 A AR P090102128A AR P090102128 A ARP090102128 A AR P090102128A AR 074151 A1 AR074151 A1 AR 074151A1
- Authority
- AR
- Argentina
- Prior art keywords
- compound
- formula
- polymorphic form
- amino
- less
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 10
- 238000000034 method Methods 0.000 title abstract 3
- 238000002360 preparation method Methods 0.000 title 1
- 238000004519 manufacturing process Methods 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 239000011541 reaction mixture Substances 0.000 abstract 2
- 239000002904 solvent Substances 0.000 abstract 2
- 239000000725 suspension Substances 0.000 abstract 2
- JCPSDGBPFXACKB-UHFFFAOYSA-N (2-amino-3-chlorophenyl)-phenylmethanone Chemical compound NC1=C(Cl)C=CC=C1C(=O)C1=CC=CC=C1 JCPSDGBPFXACKB-UHFFFAOYSA-N 0.000 abstract 1
- ZUWXHHBROGLWNH-UHFFFAOYSA-N (2-amino-5-chlorophenyl)-phenylmethanone Chemical compound NC1=CC=C(Cl)C=C1C(=O)C1=CC=CC=C1 ZUWXHHBROGLWNH-UHFFFAOYSA-N 0.000 abstract 1
- DUFFXPLJIMJGDY-UHFFFAOYSA-N 2-(2-amino-3-benzoyl-5-chlorophenyl)-2-methylsulfanylacetamide Chemical compound CSC(C(N)=O)C1=CC(Cl)=CC(C(=O)C=2C=CC=CC=2)=C1N DUFFXPLJIMJGDY-UHFFFAOYSA-N 0.000 abstract 1
- -1 2-aminobenzophenone compound Chemical class 0.000 abstract 1
- NTIZESTWPVYFNL-UHFFFAOYSA-N Methyl isobutyl ketone Chemical compound CC(C)CC(C)=O NTIZESTWPVYFNL-UHFFFAOYSA-N 0.000 abstract 1
- UIHCLUNTQKBZGK-UHFFFAOYSA-N Methyl isobutyl ketone Natural products CCC(C)C(C)=O UIHCLUNTQKBZGK-UHFFFAOYSA-N 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- QEFAQIPZVLVERP-UHFFFAOYSA-N nepafenac Chemical compound NC(=O)CC1=CC=CC(C(=O)C=2C=CC=CC=2)=C1N QEFAQIPZVLVERP-UHFFFAOYSA-N 0.000 abstract 1
- 229960001002 nepafenac Drugs 0.000 abstract 1
- 239000003960 organic solvent Substances 0.000 abstract 1
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C319/00—Preparation of thiols, sulfides, hydropolysulfides or polysulfides
- C07C319/14—Preparation of thiols, sulfides, hydropolysulfides or polysulfides of sulfides
- C07C319/20—Preparation of thiols, sulfides, hydropolysulfides or polysulfides of sulfides by reactions not involving the formation of sulfide groups
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
- C07C237/20—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
- C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
- C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
- C07C323/60—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Diabetes (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Reivindicacion 1: Un proceso para preparar un compuesto de la formula (1) donde dicho proceso comprende: i) hacer reaccionar un compuesta de la formula (2) con un compuesto N-halosuccinimida y 2-aminobenzofenona de la formula (3), en la cual R es un grupo alquilo o arilo, en presencia de un solvente orgánico, para obtener una mezcla de reaccion; ii) tratar la mezcla de reaccion con una base para obtener una mezcla que comprenda el compuesto de formula (1); y iii) de un modo opcional, aislar un compuesto de formula (1) de la mezcla. Reivindicacion 13: Compuesto de la formula (4) que tiene menos del 0,5% de 2-amino-3-benzoil-5-cloro-alfa-(metiltio)bencen-acetamida, menos del 0,5% de 2-amino-3-clorobenzofenona y menos del 0,5% de 2-amino-5-clorobenzofenona. Reivindicacion 14: Un compuesto de la forma polimorfica B de la formula (4) que tiene un patron de difraccion de polvo de rayos X (2-theta) que tiene picos característicos en aproximadamente: 4,2; 4,8; 5,9; 6,8; 7,9; 10,4; 11,3; 12,5; 13,7; 13,9; 14,4; 15,4; 16,7; 17,2; 17,7; 18,5; 19,2; 19,6; 20,1; 20,6; 21,3; 21,5; 22,2; 23,4; 24,0; 25,1; 25,7; 26,3; 26,9; 27,5; 29,5; 30,1; 32,6; 34,3; 33,8 y 37,8 grados 2-theta (+/- 0,2 grados). Reivindicacion 16: Un proceso para preparar un compuesto de la forma polimorfica B de la formula (4) proceso que comprende: i) cristalizar el compuesto de la formula (4) en un solvente que comprenda metil-isobutil-cetona, para obtener una suspension y ii) eliminar el solvente de la suspension. Reivindicacion 17: El uso del compuesto de la forma polimorfica B de la formula (4) para preparar nepafenac.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US6121508P | 2008-06-13 | 2008-06-13 | |
| US11783408P | 2008-11-25 | 2008-11-25 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR074151A1 true AR074151A1 (es) | 2010-12-29 |
Family
ID=41017177
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090102128A AR074151A1 (es) | 2008-06-13 | 2009-06-12 | Un derivado de benzoilbencenoacetamida, proceso de preparacion del mismo, forma polimorfica b de dicho compuesto, proceso de obtencion de dicha forma polimorfica b y su uso |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US8278484B2 (es) |
| EP (1) | EP2307354B1 (es) |
| AR (1) | AR074151A1 (es) |
| AT (1) | ATE555080T1 (es) |
| ES (1) | ES2386758T3 (es) |
| HR (1) | HRP20120550T1 (es) |
| WO (1) | WO2009150524A1 (es) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102438979A (zh) * | 2009-03-12 | 2012-05-02 | 麦迪凯姆股份公司 | 苯甲酰基苯乙酰胺衍生物的新型晶体 |
| US9630909B2 (en) | 2013-06-27 | 2017-04-25 | Mylan Laboratories Ltd | Process for the preparation of nepafenac |
| CN112794809B (zh) * | 2019-11-14 | 2023-12-29 | 南京济群医药科技股份有限公司 | 一种高纯度奈帕芬胺中间体的制备方法 |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4313949A (en) | 1979-09-26 | 1982-02-02 | A. H. Robins Company, Inc. | Method of producing an inhibitory effect on blood platelet aggregation |
-
2009
- 2009-06-12 US US12/483,839 patent/US8278484B2/en not_active Expired - Fee Related
- 2009-06-12 EP EP09762052A patent/EP2307354B1/en not_active Not-in-force
- 2009-06-12 WO PCT/IB2009/005918 patent/WO2009150524A1/en not_active Ceased
- 2009-06-12 ES ES09762052T patent/ES2386758T3/es active Active
- 2009-06-12 HR HRP20120550AT patent/HRP20120550T1/hr unknown
- 2009-06-12 AT AT09762052T patent/ATE555080T1/de active
- 2009-06-12 AR ARP090102128A patent/AR074151A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP2307354A1 (en) | 2011-04-13 |
| HRP20120550T1 (hr) | 2012-10-31 |
| ES2386758T3 (es) | 2012-08-29 |
| US20090312575A1 (en) | 2009-12-17 |
| US8278484B2 (en) | 2012-10-02 |
| ATE555080T1 (de) | 2012-05-15 |
| EP2307354B1 (en) | 2012-04-25 |
| WO2009150524A1 (en) | 2009-12-17 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |