UY32382A - Procedimiento para la preparación de la n-[5-(3-dimetilamino-acriloil)-2-fluoro-fenil]-n-metil-acetamida - Google Patents
Procedimiento para la preparación de la n-[5-(3-dimetilamino-acriloil)-2-fluoro-fenil]-n-metil-acetamidaInfo
- Publication number
- UY32382A UY32382A UY0001032382A UY32382A UY32382A UY 32382 A UY32382 A UY 32382A UY 0001032382 A UY0001032382 A UY 0001032382A UY 32382 A UY32382 A UY 32382A UY 32382 A UY32382 A UY 32382A
- Authority
- UY
- Uruguay
- Prior art keywords
- acetamide
- methyl
- fluoro
- phenyl
- preparation
- Prior art date
Links
Classifications
-
- 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
-
- 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
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C231/00—Preparation of carboxylic acid amides
- C07C231/12—Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C233/30—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by doubly-bound oxygen atoms
- C07C233/33—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by doubly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Se refiere a un procedimiento de preparación del compuesto N-[5-(3-dimetilamino-acriloil)-2-fluoro-fenil]-N-metil-acetamida (I), intermedio en la síntesis de compuestos con afinidad sobre el receptor GABa. La N-(5-acetil-2-fluorofenil)-n-metil-acetamida (VI) se hace reaccionar con un exceso de N,N-dimetilformamida dimetilacetal (NNDMF-DMA). La presente invención proporciona también un nuevo procedimiento para la preparación del producto con afinidad GABAa N-{2-fluoro-5-[3-(tiofeno)-2-carbonil-pirazolo[1,5-a]pirimidin-7-il]fenil}-N-metilacetamida (II), que comprende a) metilación de N-(5-acetil-2-fluorofenil)-N-acetamida (IV) con un sulfato de metilo, b) reacción del compuesto (VI) resultante con NNDMF-DMA, y c) reacción del compuesto (I) resultante con (5-amino-1H-pirazol-4-il)tiofeno-2-il-metanona (III) en ácido acético glacial. La presente invención se refiere también al nuevo intermedio (VI).
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
ES200900089 | 2009-01-13 |
Publications (1)
Publication Number | Publication Date |
---|---|
UY32382A true UY32382A (es) | 2010-07-30 |
Family
ID=42199324
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
UY0001032382A UY32382A (es) | 2009-01-13 | 2010-01-13 | Procedimiento para la preparación de la n-[5-(3-dimetilamino-acriloil)-2-fluoro-fenil]-n-metil-acetamida |
Country Status (22)
Country | Link |
---|---|
US (1) | US8163903B2 (es) |
EP (1) | EP2387557B1 (es) |
JP (1) | JP5507579B2 (es) |
KR (1) | KR101680396B1 (es) |
CN (2) | CN102282123A (es) |
AR (1) | AR075009A1 (es) |
AU (1) | AU2010205739B2 (es) |
BR (1) | BRPI1006150A2 (es) |
CA (1) | CA2747392C (es) |
CY (1) | CY1114407T1 (es) |
DK (1) | DK2387557T3 (es) |
ES (1) | ES2427972T3 (es) |
HK (1) | HK1214585A1 (es) |
MX (1) | MX2011007323A (es) |
PE (1) | PE20120111A1 (es) |
PL (1) | PL2387557T3 (es) |
PT (1) | PT2387557E (es) |
RU (1) | RU2503655C2 (es) |
SI (1) | SI2387557T1 (es) |
TW (1) | TWI389912B (es) |
UY (1) | UY32382A (es) |
WO (1) | WO2010081788A1 (es) |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN104557597B (zh) * | 2013-12-11 | 2017-08-04 | 浙江龙盛集团股份有限公司 | 一种3‑(n,n‑二取代)氨基乙酰苯胺类化合物的清洁生产方法 |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ZA831407B (en) * | 1982-03-25 | 1983-11-30 | Erba Farmitalia | Substituted ethenyl derivatives of 1h-pyrazolo(1,5-a)pyrimidine and process for their preparation |
US6399621B1 (en) * | 1999-08-10 | 2002-06-04 | American Cyanamid Company | N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1, 5-α]-pyrimidin-7-yl}phenyl)acetamide and compositions and methods related thereto |
US20050070555A1 (en) | 2001-12-21 | 2005-03-31 | Bayer Healthcare Ag | Aroyl pyridinones |
ES2222813B1 (es) * | 2003-07-24 | 2005-12-16 | Ferrer Internacional, S.A. | N-(3-(3-sustituidas-pirazolo(1,5-a)pirimidin-7-il)-fenil)-sulfonamidas y composiciones y metodos relacionados. |
EP1736475A1 (en) | 2005-06-21 | 2006-12-27 | Ferrer Internacional, S.A. | Halogenated pyrazolo[1,5-a]pyrimidines, processes, uses, compositions and intermediates |
US20080045547A1 (en) * | 2006-07-07 | 2008-02-21 | Lippa Arnold S | Salts And Co-Crystals of Pyrazolopyrimidine Compounds, Compositions Thereof And Methods For Their Production And Use |
-
2010
- 2010-01-11 BR BRPI1006150A patent/BRPI1006150A2/pt not_active Application Discontinuation
- 2010-01-11 US US13/144,066 patent/US8163903B2/en not_active Expired - Fee Related
- 2010-01-11 MX MX2011007323A patent/MX2011007323A/es active IP Right Grant
- 2010-01-11 PE PE2011001315A patent/PE20120111A1/es active IP Right Grant
- 2010-01-11 CA CA2747392A patent/CA2747392C/en not_active Expired - Fee Related
- 2010-01-11 AU AU2010205739A patent/AU2010205739B2/en not_active Ceased
- 2010-01-11 WO PCT/EP2010/050235 patent/WO2010081788A1/en active Application Filing
- 2010-01-11 SI SI201030316T patent/SI2387557T1/sl unknown
- 2010-01-11 EP EP10700974.8A patent/EP2387557B1/en not_active Not-in-force
- 2010-01-11 RU RU2011133958/04A patent/RU2503655C2/ru not_active IP Right Cessation
- 2010-01-11 PT PT107009748T patent/PT2387557E/pt unknown
- 2010-01-11 KR KR1020117015699A patent/KR101680396B1/ko active IP Right Grant
- 2010-01-11 DK DK10700974.8T patent/DK2387557T3/da active
- 2010-01-11 CN CN2010800043825A patent/CN102282123A/zh active Pending
- 2010-01-11 CN CN201510351862.3A patent/CN104945272A/zh active Pending
- 2010-01-11 AR ARP100100060A patent/AR075009A1/es not_active Application Discontinuation
- 2010-01-11 ES ES10700974T patent/ES2427972T3/es active Active
- 2010-01-11 PL PL10700974T patent/PL2387557T3/pl unknown
- 2010-01-11 JP JP2011544885A patent/JP5507579B2/ja active Active
- 2010-01-12 TW TW099100648A patent/TWI389912B/zh not_active IP Right Cessation
- 2010-01-13 UY UY0001032382A patent/UY32382A/es not_active Application Discontinuation
-
2013
- 2013-09-17 CY CY20131100802T patent/CY1114407T1/el unknown
-
2015
- 2015-10-29 HK HK15110697.8A patent/HK1214585A1/zh unknown
Also Published As
Publication number | Publication date |
---|---|
KR101680396B1 (ko) | 2016-11-28 |
CN104945272A (zh) | 2015-09-30 |
JP2012515149A (ja) | 2012-07-05 |
US20110275809A1 (en) | 2011-11-10 |
BRPI1006150A2 (pt) | 2018-01-16 |
KR20110108346A (ko) | 2011-10-05 |
TWI389912B (zh) | 2013-03-21 |
AR075009A1 (es) | 2011-03-02 |
RU2011133958A (ru) | 2013-02-20 |
WO2010081788A1 (en) | 2010-07-22 |
JP5507579B2 (ja) | 2014-05-28 |
SI2387557T1 (sl) | 2013-12-31 |
RU2503655C2 (ru) | 2014-01-10 |
EP2387557B1 (en) | 2013-06-19 |
CN102282123A (zh) | 2011-12-14 |
PL2387557T3 (pl) | 2013-12-31 |
CA2747392A1 (en) | 2010-07-22 |
TW201026704A (en) | 2010-07-16 |
ES2427972T3 (es) | 2013-11-05 |
PT2387557E (pt) | 2013-09-11 |
CY1114407T1 (el) | 2016-08-31 |
US8163903B2 (en) | 2012-04-24 |
CA2747392C (en) | 2016-10-18 |
AU2010205739A1 (en) | 2011-07-21 |
EP2387557A1 (en) | 2011-11-23 |
HK1214585A1 (zh) | 2016-07-29 |
AU2010205739B2 (en) | 2015-12-10 |
PE20120111A1 (es) | 2012-02-10 |
MX2011007323A (es) | 2011-07-29 |
DK2387557T3 (da) | 2013-09-08 |
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Legal Events
Date | Code | Title | Description |
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109 | Application deemed to be withdrawn |
Effective date: 20201221 |