HUP0301463A2 - Eljárás szubsztituált oktanoil-amid-származékok elżállítására, valamint az elżállításhoz alkalmazott közbensż termékek - Google Patents
Eljárás szubsztituált oktanoil-amid-származékok elżállítására, valamint az elżállításhoz alkalmazott közbensż termékekInfo
- Publication number
- HUP0301463A2 HUP0301463A2 HU0301463A HUP0301463A HUP0301463A2 HU P0301463 A2 HUP0301463 A2 HU P0301463A2 HU 0301463 A HU0301463 A HU 0301463A HU P0301463 A HUP0301463 A HU P0301463A HU P0301463 A2 HUP0301463 A2 HU P0301463A2
- Authority
- HU
- Hungary
- Prior art keywords
- alkyl
- general formula
- compound
- carbon atom
- alkoxy
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 3
- 239000000543 intermediate Substances 0.000 title 1
- LTHCSWBWNVGEFE-UHFFFAOYSA-N octanamide Chemical class CCCCCCCC(N)=O LTHCSWBWNVGEFE-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 8
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 6
- 229910052799 carbon Inorganic materials 0.000 abstract 5
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 1
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- -1 amine compound Chemical class 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- IVRMZWNICZWHMI-UHFFFAOYSA-N azide group Chemical group [N-]=[N+]=[N-] IVRMZWNICZWHMI-UHFFFAOYSA-N 0.000 abstract 1
- 230000004531 blood pressure lowering effect Effects 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 239000013067 intermediate product Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 abstract 1
- 239000007858 starting material Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C231/00—Preparation of carboxylic acid amides
- C07C231/02—Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D207/33—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C247/00—Compounds containing azido groups
- C07C247/02—Compounds containing azido groups with azido groups bound to acyclic carbon atoms of a carbon skeleton
- C07C247/12—Compounds containing azido groups with azido groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by carboxyl groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
- C07C57/30—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms containing six-membered aromatic rings
- C07C57/42—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms containing six-membered aromatic rings having unsaturation outside the rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C59/40—Unsaturated compounds
- C07C59/58—Unsaturated compounds containing ether groups, groups, groups, or groups
- C07C59/64—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
- C07C69/66—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
- C07C69/73—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids
- C07C69/734—Ethers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
- C07D303/02—Compounds containing oxirane rings
- C07D303/38—Compounds containing oxirane rings with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/26—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D307/30—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
- C07D307/32—Oxygen atoms
- C07D307/33—Oxygen atoms in position 2, the oxygen atom being in its keto or unsubstituted enol form
Abstract
A találmány tárgyát eljárás képezi az (I) általános képletű vegyületekelőállítására. Az (I) általános képletben a szubsztituensek jelentéseR1 és R2 jelentése egymástól függetlenül hidrogénatom, 1-6 szénatomosalkil-, 1-6 szénatomos halogénalkil-, 1-6 szénatomos alkoxi-, 1-6szénatomos alkoxi-(1-6 szénatomos alkil)- vagy 1-6 szénatomos alkoxi-(1-6 szénatomos alkil)-oxi-csoport, R3 jelentése 1-6 szénatomosalkilcsoport, R4 jelentése 1-6 szénatomos alkilcsoport, továbbá R5jelentése 1-6 szénatomos alkil-, 1-6 szénatomos hidroxi-alkil-, 1-6szénatomos alkoxi-(1-6 szénatomos alkil)-, 1-6 szénatomos alkanoil-oxi-(1-6 szénatomos alkil)-, 1-6 szénatomos amino-alkil-, 1-6szénatomos alkil-amino-(1-6 szénatomos alkil)-, di(1-6 szénatomosalkil)-amino-(1-6 szénatomos alkil)-, 1-6 szénatomos alkanoil-amido-(1-6 szénatomos alkil)-, HO(O)C-(1-6 szénatomos alkil)-, 1-6szénatomos alkil-O-(O)C-(1-6 szénatomos alkil)-, H2N-C(O)-(1-6szénatomos alkil)-, 1-6 szénatomos alkil-HN-C(O)-(1-6 szénatomosalkil)- vagy (1-6 szénatomos alkil)2N-C(O)-(1-6 szénatomos alkil)-csoport. Az (I) általános képletű vegyületek vérnyomást csökkentőhatással rendelkeznek és mint ilyenek nyernek alkalmazást. Az (I)általános képletű vegyületeket oly módon állítják elő, hogy a) (II)általános képletű vegyületet R5-NH2 általános képletű amin-vegyülettel reagáltatnak, amikor is (III) általános képletű vegyületetkapnak, majd b) az így nyert (III) általános képletű vegyületben lévőazidcsoportot aminocsoporttá redukálják és az így keletkezett (I)általános képletű vegyületet elkülönítik, adott esetben sóképző savhozzáadásával. A találmány tárgyához tartozik a kiindulásivegyületként alkalmazott (II) általános képletű vegyület előállításáraszolgáló eljárás, valamint némely új közbenső termék is. Ó
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CH13292000 | 2000-07-05 | ||
CH24502000 | 2000-12-15 | ||
PCT/CH2001/000399 WO2002002508A1 (en) | 2000-07-05 | 2001-06-26 | Process for the preparation of substituted octanoyl amides |
Publications (3)
Publication Number | Publication Date |
---|---|
HUP0301463A2 true HUP0301463A2 (hu) | 2003-09-29 |
HUP0301463A3 HUP0301463A3 (en) | 2008-03-28 |
HU228526B1 HU228526B1 (hu) | 2013-03-28 |
Family
ID=25738979
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0301463A HU228526B1 (hu) | 2000-07-05 | 2001-06-26 | Eljárás szubsztituált oktanoil-amid-származékok elõállítására, valamint az elõállításhoz alkalmazott közbensõ termékek |
Country Status (24)
Country | Link |
---|---|
US (1) | US6730798B2 (hu) |
EP (1) | EP1296935B1 (hu) |
JP (1) | JP4900755B2 (hu) |
KR (1) | KR100690471B1 (hu) |
CN (1) | CN100482636C (hu) |
AR (1) | AR029564A1 (hu) |
AT (1) | ATE426592T1 (hu) |
AU (2) | AU2001273763B2 (hu) |
BR (1) | BR0112362B1 (hu) |
CA (1) | CA2414847C (hu) |
CY (1) | CY1109110T1 (hu) |
DE (1) | DE60138099D1 (hu) |
DK (1) | DK1296935T3 (hu) |
ES (1) | ES2322547T3 (hu) |
HK (1) | HK1093201A1 (hu) |
HU (1) | HU228526B1 (hu) |
IL (4) | IL153717A0 (hu) |
MX (1) | MXPA02012628A (hu) |
NO (1) | NO328105B1 (hu) |
NZ (1) | NZ523088A (hu) |
PL (1) | PL212898B1 (hu) |
PT (1) | PT1296935E (hu) |
TW (1) | TWI289551B (hu) |
WO (1) | WO2002002508A1 (hu) |
Families Citing this family (34)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20060154926A1 (en) * | 2002-06-11 | 2006-07-13 | Elan Pharmaceuticals, Inc. | Methods of treating alzheimer's disease using aryl alkanoic acid amides |
GB0419361D0 (en) | 2004-08-31 | 2004-10-06 | Novartis Ag | Organic compounds |
GB0511686D0 (en) | 2005-06-08 | 2005-07-13 | Novartis Ag | Organic compounds |
RU2470018C2 (ru) * | 2005-07-11 | 2012-12-20 | Новартис Аг | Новые производные пирокатехина |
GB0519764D0 (en) | 2005-09-28 | 2005-11-09 | Novartis Ag | Organic compounds |
GB2431649A (en) * | 2005-10-25 | 2007-05-02 | Novartis Ag | Alternative synthesis of aryl-octanoyl amide compounds |
GB2431645A (en) * | 2005-10-25 | 2007-05-02 | Novartis Ag | Alternative synthesis of aryl-octanoyl amide compounds |
DE102005052195A1 (de) | 2005-10-28 | 2007-05-03 | Reuter Chemischer Apparatebau Kg | Verfahren zur Herstellung von chiralen Octensäurederivaten |
GB0605688D0 (en) | 2006-03-21 | 2006-05-03 | Novartis Ag | Organic compounds |
PE20081157A1 (es) * | 2006-11-07 | 2008-09-26 | Novartis Ag | Forma cristalina de hemifumarato de alisquireno |
BRPI0718701A2 (pt) * | 2006-11-09 | 2013-12-31 | Novartis Ag | Sal de alisquireno com ácido orótico |
EP1958666A1 (en) | 2007-02-13 | 2008-08-20 | Speedel Experimenta AG | Heterocyclic-substituted alkanamides as therapeutic compounds |
DE102007049039A1 (de) | 2007-10-11 | 2009-04-16 | Reuter Chemischer Apparatebau Kg | Verfahren zur Herstellung von 8-Hydrazino-8-Aryl-Octanoylderivaten und deren Verwendung |
EP2220031A1 (en) * | 2007-11-13 | 2010-08-25 | Teva Pharmaceutical Industries Ltd. | Polymorphic forms of aliskiren hemifumarate and process for preparation thereof |
EP2062874B1 (en) | 2007-11-20 | 2014-12-17 | KRKA, tovarna zdravil, d.d., Novo mesto | Process and intermediates for the preparation of aliskiren |
WO2009143423A1 (en) * | 2008-05-23 | 2009-11-26 | Teva Pharmaceutical Industries Ltd. | Aliskiren monofumarate and processes for preparation thereof |
EP2189442B1 (en) | 2008-11-20 | 2014-10-01 | Krka Tovarna Zdravil, D.D., Novo Mesto | Process and intermediates for the preparation of aliskiren |
WO2010089105A2 (en) | 2009-02-05 | 2010-08-12 | Krka, Tovarna Zdravil, D.D., Novo Mesto | Moisture-activated granulation process |
EP2273990A2 (en) * | 2009-02-05 | 2011-01-19 | Teva Pharmaceutical Industries Ltd. | Solid state forms of aliskiren compounds |
WO2011028919A2 (en) | 2009-09-03 | 2011-03-10 | Teva Pharmaceutical Industries Ltd. | Solid forms of aliskiren hemifumarate and processes for preparation thereof |
WO2011051853A1 (en) | 2009-10-29 | 2011-05-05 | CarboDesign LLC | Manufacturing process for preparing enaniomerically pure 8- aryloctanoic acid derivatives such as aliskiren |
US20110113995A1 (en) * | 2009-11-13 | 2011-05-19 | Lindsay Corporation | Method and apparatus for planting and irrigation |
WO2011148392A1 (en) * | 2010-05-28 | 2011-12-01 | Msn Laboratories Limited | Process for the preparation of (2s,4s,5s,7s)-n-(2-carbamyl-2- methylpropyl)-5-amino-4-hydroxy-2,7-diisopropyl-8-[4-methoxy-3-(3- methoxypropoxy)phenyl]-octanamide hemifumarate and its intermediates thereof |
WO2012052829A1 (en) | 2010-10-19 | 2012-04-26 | Matrix Laboratories Ltd | Synthesis of aliskiren |
ITMI20110893A1 (it) * | 2011-05-19 | 2012-11-20 | Chemelectiva S R L | Processi ed intermedi per la sintesi di aliskiren |
EP2551260A1 (en) | 2011-07-28 | 2013-01-30 | Chemo Ibérica, S.A. | Chemical process for opening ring compounds |
US8703976B2 (en) | 2011-10-02 | 2014-04-22 | Milan Soukup | Manufacturing process for 8-aryloctanoic acids such as Aliskiren |
WO2013118138A1 (en) | 2011-12-13 | 2013-08-15 | Laboratories Ltd Mylan | Novel process for the preparation of renin inhibitors |
US9090537B2 (en) | 2012-02-17 | 2015-07-28 | Mylan Laboratories Limited | Process for the preparation of aliskiren |
WO2013124868A2 (en) | 2012-02-21 | 2013-08-29 | Mylan Laboratories Limited | Solid form of aliskiren intermediate |
WO2013144979A1 (en) | 2012-03-28 | 2013-10-03 | Maylan Laboratories Ltd | Process for the preparation of aliskiren |
WO2013171767A1 (en) | 2012-05-18 | 2013-11-21 | Mylan Laboratories Limited | An improved process for the preparation of aliskiren |
CN104876832B (zh) * | 2014-02-28 | 2016-12-07 | 华润双鹤药业股份有限公司 | 阿利吉仑的4-位差向异构体、其制备方法及用途 |
CN106146339B (zh) * | 2015-04-23 | 2018-02-23 | 华润双鹤药业股份有限公司 | 阿利吉仑的5‑位差向异构体、其制备方法及用途 |
Family Cites Families (8)
Publication number | Priority date | Publication date | Assignee | Title |
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US4492799A (en) * | 1979-07-02 | 1985-01-08 | Union Carbide Corporation | Halo-4-alkenoic acids and their use as pesticidal intermediates |
FR2666757B1 (fr) * | 1990-09-14 | 1992-12-18 | Usinor Sacilor | Virole pour cylindre de coulee continue des metaux, notamment de l'acier, entre cylindres ou sur un cylindre. |
MY119161A (en) * | 1994-04-18 | 2005-04-30 | Novartis Ag | Delta-amino-gamma-hydroxy-omega-aryl-alkanoic acid amides with enzyme especially renin inhibiting activities |
US5606078A (en) | 1994-04-18 | 1997-02-25 | Ciba-Geigy Corporation | 3,5-Disubstituted tetrahydrofuran-2-ones |
US5659065A (en) * | 1994-04-18 | 1997-08-19 | Novartis Corporation | Alpha-aminoalkanoic acids and reduction products |
WO1996002340A1 (de) * | 1994-07-18 | 1996-02-01 | Siemens Aktiengesellschaft | Giesswalzen-verschleissschutzschicht |
WO1998052706A1 (de) * | 1997-05-23 | 1998-11-26 | Voest-Alpine Industrieanlagenbau Gmbh | Giesswalze für eine dünnband-stranggiessanlage |
ES2218173T3 (es) * | 1999-07-29 | 2004-11-16 | Speedel Pharma Ag | Acidos 2-alquil-5-halogano-pent-4-enocarboxilicos y su fabricacion. |
-
2001
- 2001-06-26 ES ES01940047T patent/ES2322547T3/es not_active Expired - Lifetime
- 2001-06-26 AU AU2001273763A patent/AU2001273763B2/en not_active Ceased
- 2001-06-26 WO PCT/CH2001/000399 patent/WO2002002508A1/en active Application Filing
- 2001-06-26 NZ NZ523088A patent/NZ523088A/en not_active IP Right Cessation
- 2001-06-26 US US10/312,987 patent/US6730798B2/en not_active Expired - Lifetime
- 2001-06-26 DE DE60138099T patent/DE60138099D1/de not_active Expired - Lifetime
- 2001-06-26 CN CNB018122817A patent/CN100482636C/zh not_active Expired - Lifetime
- 2001-06-26 JP JP2002507765A patent/JP4900755B2/ja not_active Expired - Lifetime
- 2001-06-26 AT AT01940047T patent/ATE426592T1/de active
- 2001-06-26 HU HU0301463A patent/HU228526B1/hu not_active IP Right Cessation
- 2001-06-26 CA CA002414847A patent/CA2414847C/en not_active Expired - Fee Related
- 2001-06-26 KR KR1020027017207A patent/KR100690471B1/ko active IP Right Grant
- 2001-06-26 IL IL15371701A patent/IL153717A0/xx unknown
- 2001-06-26 PL PL358887A patent/PL212898B1/pl unknown
- 2001-06-26 EP EP01940047A patent/EP1296935B1/en not_active Expired - Lifetime
- 2001-06-26 PT PT01940047T patent/PT1296935E/pt unknown
- 2001-06-26 AU AU7376301A patent/AU7376301A/xx active Pending
- 2001-06-26 BR BRPI0112362-9B1A patent/BR0112362B1/pt not_active IP Right Cessation
- 2001-06-26 MX MXPA02012628A patent/MXPA02012628A/es active IP Right Grant
- 2001-06-26 DK DK01940047T patent/DK1296935T3/da active
- 2001-06-29 TW TW090115929A patent/TWI289551B/zh not_active IP Right Cessation
- 2001-07-04 AR ARP010103194A patent/AR029564A1/es active IP Right Grant
-
2002
- 2002-12-27 IL IL153717A patent/IL153717A/en not_active IP Right Cessation
-
2003
- 2003-01-02 NO NO20030012A patent/NO328105B1/no not_active IP Right Cessation
-
2006
- 2006-12-19 HK HK06113953.2A patent/HK1093201A1/xx not_active IP Right Cessation
-
2007
- 2007-11-29 IL IL187795A patent/IL187795A/en not_active IP Right Cessation
- 2007-11-29 IL IL187796A patent/IL187796A/en not_active IP Right Cessation
-
2009
- 2009-05-28 CY CY20091100571T patent/CY1109110T1/el unknown
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