AR065858A1 - Metodo para preparar el inhibidor de triptasa [ 4-(5-aminoetil-2-fluoro-fenil)-piperidin-1-il]-(4-bromo-3-metil-5-propoxi-tiofen-2-il)-metanona. - Google Patents
Metodo para preparar el inhibidor de triptasa [ 4-(5-aminoetil-2-fluoro-fenil)-piperidin-1-il]-(4-bromo-3-metil-5-propoxi-tiofen-2-il)-metanona.Info
- Publication number
- AR065858A1 AR065858A1 ARP080101260A ARP080101260A AR065858A1 AR 065858 A1 AR065858 A1 AR 065858A1 AR P080101260 A ARP080101260 A AR P080101260A AR P080101260 A ARP080101260 A AR P080101260A AR 065858 A1 AR065858 A1 AR 065858A1
- Authority
- AR
- Argentina
- Prior art keywords
- piperidin
- bromo
- methyl
- fluoro
- phenyl
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- -1 [4- (5-aminomethyl-2-fluoro-phenyl) -piperidin-1yl] - (4-bromo-3-methyl-5-propoxy-thiophene-2-yl) Chemical group 0.000 abstract 3
- VWFVJVPPXXCWAW-UHFFFAOYSA-N 4-bromo-3-methyl-5-propoxythiophene-2-carboxylic acid Chemical compound CCCOC=1SC(C(O)=O)=C(C)C=1Br VWFVJVPPXXCWAW-UHFFFAOYSA-N 0.000 abstract 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 abstract 1
- IFWLUOOAWLUBQN-UHFFFAOYSA-N [4-[5-(aminomethyl)-2-fluorophenyl]piperidin-1-yl]-(4-bromo-3-methyl-5-propoxythiophen-2-yl)methanone Chemical compound BrC1=C(OCCC)SC(C(=O)N2CCC(CC2)C=2C(=CC=C(CN)C=2)F)=C1C IFWLUOOAWLUBQN-UHFFFAOYSA-N 0.000 abstract 1
- 230000008878 coupling Effects 0.000 abstract 1
- 238000010168 coupling process Methods 0.000 abstract 1
- 238000005859 coupling reaction Methods 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- CJDDAVPYKYRBPT-UHFFFAOYSA-N n-[[3-[1-(4-bromo-3-methyl-5-propoxythiophene-2-carbonyl)piperidin-4-yl]-4-fluorophenyl]methyl]-2,2,2-trifluoroacetamide Chemical compound BrC1=C(OCCC)SC(C(=O)N2CCC(CC2)C=2C(=CC=C(CNC(=O)C(F)(F)F)C=2)F)=C1C CJDDAVPYKYRBPT-UHFFFAOYSA-N 0.000 abstract 1
- 239000002904 solvent Substances 0.000 abstract 1
- 150000003512 tertiary amines Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Reivindicacion 1: Procedimiento para preparar [4-(5-aminometil-2-fluoro-fenil)-piperidin-1il]-(4-bromo-3-metil-5-propoxi-tiofen-2-il)-meta nona que comprende acoplar por imitacion el éster de2,5-dioxo-pirrolidin-1-ilo de ácido 4-bromo-3-metil-5-propoxitiofeno-2-carboxílico con hidrocloruro de 2,2,2-trifluoro-N-(4-fluoro-3-piperidin-4-il-bencil)-acetamida y una base fuerte o una base amina terciaria en un disolvente alcoholico para producir 2,2,2-trifluoro-N-{3-[1-(4-Bromo-3-metil-5-propoxi-tiofeno-2-carbonil)-piperidin-4-il]-4-fluoro-bencil}-acetamida y desproteger la 2,2,2-trifluoro-N-{3-[1-(4-Bromo-3-metil-5-propoxi-tiofeno-2-carbonil)-piperidin-4-il]-4-fluro-bencil}-acetamida con una base para producir [4-(5-aminometil-2-fluoro-fenil)-piperidin-1-il]-(4-bromo -3-metil-5-propoxy-thiophen-2-il)-metanona
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US90884407P | 2007-03-29 | 2007-03-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR065858A1 true AR065858A1 (es) | 2009-07-08 |
Family
ID=39535396
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080101260A AR065858A1 (es) | 2007-03-29 | 2008-03-27 | Metodo para preparar el inhibidor de triptasa [ 4-(5-aminoetil-2-fluoro-fenil)-piperidin-1-il]-(4-bromo-3-metil-5-propoxi-tiofen-2-il)-metanona. |
Country Status (3)
| Country | Link |
|---|---|
| AR (1) | AR065858A1 (es) |
| TW (1) | TW200904811A (es) |
| WO (1) | WO2008121666A1 (es) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HRP20151338T1 (hr) * | 2008-08-22 | 2016-01-15 | Sanofi | [4-(5-aminometil-2-fluoro-fenil)-piperidin-1-il]-[7-fluoro-1-(2-metoksi-etil)-4trifluorometoksi-1h-indol-3-il]metanon kao inhibitor triptaze mastocita |
| GB0905955D0 (en) | 2009-04-06 | 2009-05-20 | Respivert Ltd | Novel compounds |
| JP5787977B2 (ja) | 2010-04-08 | 2015-09-30 | レスピバート・リミテツド | Ｐ３８ｍａｐキナーゼ阻害剤 |
| EP2582700B1 (en) | 2010-06-17 | 2016-11-02 | Respivert Limited | Respiratory formulations containing p38 mapk inhibitors |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DOP2005000039A (es) * | 2004-03-26 | 2005-10-31 | Aventis Pharma Inc | Hidrocloruro de [4-(5-aminometil-2-fluoro-fenil)- piperidin-1-il]-(4-bomo-3-metil-5-propoxi-tiofen-2-il)-metanona como un inhibidor de la triptasa de mastocitos |
-
2008
- 2008-03-27 AR ARP080101260A patent/AR065858A1/es not_active Application Discontinuation
- 2008-03-27 WO PCT/US2008/058341 patent/WO2008121666A1/en not_active Ceased
- 2008-03-28 TW TW097111154A patent/TW200904811A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2008121666A1 (en) | 2008-10-09 |
| TW200904811A (en) | 2009-02-01 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |