IN2014DN08922A - - Google Patents
Info
- Publication number
- IN2014DN08922A IN2014DN08922A IN8922DEN2014A IN2014DN08922A IN 2014DN08922 A IN2014DN08922 A IN 2014DN08922A IN 8922DEN2014 A IN8922DEN2014 A IN 8922DEN2014A IN 2014DN08922 A IN2014DN08922 A IN 2014DN08922A
- Authority
- IN
- India
- Prior art keywords
- pyrazine
- difluoromethyl
- action
- hibitory
- chloropyrazine
- Prior art date
Links
- IHYMWNUBROPCOP-UHFFFAOYSA-N 5-(difluoromethyl)pyrazine-2-carboxamide Chemical compound NC(=O)C1=CN=C(C(F)F)C=N1 IHYMWNUBROPCOP-UHFFFAOYSA-N 0.000 abstract 1
- ABKZAJKWQBRNOR-UHFFFAOYSA-N 5-[carboxy(difluoro)methyl]pyrazine-2-carboxylic acid Chemical compound OC(=O)C1=CN=C(C(F)(F)C(O)=O)C=N1 ABKZAJKWQBRNOR-UHFFFAOYSA-N 0.000 abstract 1
- FXJOTWLLDJYKAG-UHFFFAOYSA-N 5-chloropyrazine-2-carboxylic acid Chemical compound OC(=O)C1=CN=C(Cl)C=N1 FXJOTWLLDJYKAG-UHFFFAOYSA-N 0.000 abstract 1
- 102100021257 Beta-secretase 1 Human genes 0.000 abstract 1
- 101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 238000010276 construction Methods 0.000 abstract 1
- 230000000911 decarboxylating effect Effects 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000002994 raw material Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
5-(Difluoromethyl)pyrazine-2-carboxilic acid, which is a raw material for the construction of 5- (difluoromethyl)pyrazine-2-carboxamide, which is a common partial structural motif of the compound having an A production in hibitory action or a BACE1 inhibitory action, can be industrially advantageously produced by decarboxylating 5- [carboxy(difluoro)methyl]pyrazine-2-carboxylic acid, which is obtainable from 5-chloropyrazine-2-carboxylate.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261639362P | 2012-04-27 | 2012-04-27 | |
| PCT/JP2013/062863 WO2013162065A1 (en) | 2012-04-27 | 2013-04-25 | Method for producing 5-(difluoromethyl)pyrazine-2-carboxilic acid and production intermediate thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IN2014DN08922A true IN2014DN08922A (en) | 2015-05-22 |
Family
ID=49483351
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IN8922DEN2014 IN2014DN08922A (en) | 2012-04-27 | 2013-04-25 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US9227942B2 (en) |
| EP (1) | EP2841423B1 (en) |
| JP (1) | JP6118817B2 (en) |
| CN (1) | CN104245680B (en) |
| BR (1) | BR112014026474A2 (en) |
| CA (1) | CA2871264A1 (en) |
| ES (1) | ES2615304T3 (en) |
| HU (1) | HUE030534T2 (en) |
| IL (1) | IL235161A0 (en) |
| IN (1) | IN2014DN08922A (en) |
| MX (1) | MX2014012683A (en) |
| RU (1) | RU2014142545A (en) |
| SG (1) | SG11201406589PA (en) |
| WO (1) | WO2013162065A1 (en) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO3318B1 (en) | 2013-06-18 | 2019-03-13 | Lilly Co Eli | Bace inhibitors |
| CN115087636A (en) * | 2020-02-06 | 2022-09-20 | Ａｇｃ株式会社 | Process for producing aromatic heterocyclic-substituted difluoroacetic acid derivative |
| CN112645890B (en) * | 2020-12-25 | 2022-08-12 | 江苏广域化学有限公司 | Synthesis method of 2-pyrazine carboxylic ester compound |
| JPWO2023017798A1 (en) * | 2021-08-11 | 2023-02-16 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2007208494A1 (en) | 2006-01-12 | 2007-08-02 | Merck Sharp & Dohme Corp. | Fluorinated arylamide derivatives |
| ES2548774T3 (en) * | 2008-01-18 | 2015-10-20 | Eisai R&D Management Co., Ltd. | Condensed aminodihydrotiazine derivative |
| WO2010009155A2 (en) * | 2008-07-14 | 2010-01-21 | Gilead Colorado, Inc. | Fused heterocyclyc inhibitor compounds |
| JP5666304B2 (en) | 2008-09-30 | 2015-02-12 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | Novel condensed aminodihydrothiazine derivatives |
| AR077277A1 (en) | 2009-07-09 | 2011-08-17 | Lilly Co Eli | BICYCLE COMPOUNDS (1,3) TIAZIN-2-AMINA PHARMACEUTICAL FORMULATION THAT INCLUDES IT AND ITS USE FOR THE MANUFACTURE OF A USEFUL MEDICINAL PRODUCT FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
| GB0912777D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydropyrimidone derivatives |
| GB0912778D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
| JP5696355B2 (en) * | 2009-11-18 | 2015-04-08 | セントラル硝子株式会社 | Method for producing aromatic difluoromethyl compound |
| US8673894B2 (en) | 2010-05-07 | 2014-03-18 | Hoffmann-La Roche Inc. | 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds |
| JP5679855B2 (en) * | 2011-02-14 | 2015-03-04 | 国立大学法人群馬大学 | Method for producing difluoromethylated heteroaryl compound |
-
2013
- 2013-04-25 IN IN8922DEN2014 patent/IN2014DN08922A/en unknown
- 2013-04-25 CN CN201380021262.XA patent/CN104245680B/en active Active
- 2013-04-25 CA CA2871264A patent/CA2871264A1/en not_active Abandoned
- 2013-04-25 US US14/396,261 patent/US9227942B2/en active Active
- 2013-04-25 SG SG11201406589PA patent/SG11201406589PA/en unknown
- 2013-04-25 BR BR112014026474A patent/BR112014026474A2/en not_active Application Discontinuation
- 2013-04-25 ES ES13781634.4T patent/ES2615304T3/en active Active
- 2013-04-25 HU HUE13781634A patent/HUE030534T2/en unknown
- 2013-04-25 JP JP2014547207A patent/JP6118817B2/en not_active Expired - Fee Related
- 2013-04-25 MX MX2014012683A patent/MX2014012683A/en unknown
- 2013-04-25 EP EP13781634.4A patent/EP2841423B1/en active Active
- 2013-04-25 RU RU2014142545A patent/RU2014142545A/en unknown
- 2013-04-25 WO PCT/JP2013/062863 patent/WO2013162065A1/en not_active Ceased
-
2014
- 2014-10-19 IL IL235161A patent/IL235161A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| SG11201406589PA (en) | 2014-11-27 |
| CA2871264A1 (en) | 2013-10-31 |
| HUE030534T2 (en) | 2017-05-29 |
| BR112014026474A2 (en) | 2017-06-27 |
| CN104245680B (en) | 2016-11-23 |
| JP6118817B2 (en) | 2017-04-19 |
| WO2013162065A1 (en) | 2013-10-31 |
| ES2615304T3 (en) | 2017-06-06 |
| US9227942B2 (en) | 2016-01-05 |
| IL235161A0 (en) | 2014-12-31 |
| EP2841423A1 (en) | 2015-03-04 |
| EP2841423A4 (en) | 2015-09-09 |
| JP2015514676A (en) | 2015-05-21 |
| MX2014012683A (en) | 2015-01-16 |
| EP2841423B1 (en) | 2016-11-30 |
| US20150087836A1 (en) | 2015-03-26 |
| RU2014142545A (en) | 2016-06-27 |
| CN104245680A (en) | 2014-12-24 |
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