ATE406346T1 - Herstellung von n-substituierten 2,7-dialkyl-4- hydroxy-5-amino-8-aryl-octanoylamiden - Google Patents
Herstellung von n-substituierten 2,7-dialkyl-4- hydroxy-5-amino-8-aryl-octanoylamidenInfo
- Publication number
- ATE406346T1 ATE406346T1 AT00940108T AT00940108T ATE406346T1 AT E406346 T1 ATE406346 T1 AT E406346T1 AT 00940108 T AT00940108 T AT 00940108T AT 00940108 T AT00940108 T AT 00940108T AT E406346 T1 ATE406346 T1 AT E406346T1
- Authority
- AT
- Austria
- Prior art keywords
- sub
- alkyl
- alkoxy
- formula
- substituted
- Prior art date
Links
- 125000000217 alkyl group Chemical group 0.000 abstract 23
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 2
- 150000001412 amines Chemical class 0.000 abstract 1
- IVRMZWNICZWHMI-UHFFFAOYSA-N azide group Chemical group [N-]=[N+]=[N-] IVRMZWNICZWHMI-UHFFFAOYSA-N 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 238000007245 halolactonization reaction Methods 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 238000007142 ring opening reaction Methods 0.000 abstract 1
- -1 tetramethylene, pentamethylene, 3-oxa-1,5-pentylene Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
- C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
- C07D295/182—Radicals derived from carboxylic acids
- C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
-
- 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
- C07C233/02—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
- C07C233/09—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to carbon atoms of an acyclic unsaturated carbon skeleton
-
- 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
- C07C233/16—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 singly-bound oxygen atoms
- C07C233/17—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 singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
- C07C233/20—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 singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a carbon atom of an acyclic unsaturated carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C235/32—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
- C07C235/34—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic 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
- C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
- C07C51/06—Preparation of carboxylic acids or their salts, halides or anhydrides from carboxylic acid amides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
- C07C57/52—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms containing halogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
- C07C57/64—Acyl halides
- C07C57/76—Acyl halides containing halogen outside the carbonyl halide groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
- C07C69/62—Halogen-containing esters
- C07C69/65—Halogen-containing esters of unsaturated acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings 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
- C07D263/18—Oxygen atoms
- C07D263/20—Oxygen atoms attached in position 2
- C07D263/22—Oxygen atoms attached in position 2 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to other ring carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Furan Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CH140199 | 1999-07-29 | ||
| CH442000 | 2000-01-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE406346T1 true ATE406346T1 (de) | 2008-09-15 |
Family
ID=25687539
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT00940109T ATE265415T1 (de) | 1999-07-29 | 2000-07-13 | 2-alkyl-5-halogen-pent-4-encarbonsäuren und deren herstellung |
| AT00940108T ATE406346T1 (de) | 1999-07-29 | 2000-07-13 | Herstellung von n-substituierten 2,7-dialkyl-4- hydroxy-5-amino-8-aryl-octanoylamiden |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT00940109T ATE265415T1 (de) | 1999-07-29 | 2000-07-13 | 2-alkyl-5-halogen-pent-4-encarbonsäuren und deren herstellung |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US6777574B1 (enExample) |
| EP (2) | EP1200384B1 (enExample) |
| JP (2) | JP4580606B2 (enExample) |
| AT (2) | ATE265415T1 (enExample) |
| AU (2) | AU5518500A (enExample) |
| DE (2) | DE50006271D1 (enExample) |
| DK (2) | DK1200390T3 (enExample) |
| ES (2) | ES2312346T3 (enExample) |
| PT (2) | PT1200390E (enExample) |
| WO (2) | WO2001009083A1 (enExample) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2414847C (en) | 2000-07-05 | 2009-06-16 | Speedel Pharma Ag | Process for the preparation of substituted octanoyl amides |
| MXPA03010394A (es) * | 2001-05-15 | 2004-03-09 | Speedel Pharma Ag | Proceso para la preparacion de esteres de acido carboxilico substituidos por hidrolisis enzimatica. |
| US20060154926A1 (en) * | 2002-06-11 | 2006-07-13 | Elan Pharmaceuticals, Inc. | Methods of treating alzheimer's disease using aryl alkanoic acid amides |
| WO2004052828A1 (ja) * | 2002-12-09 | 2004-06-24 | Asahi Glass Company, Limited | （４ｅ）−５−クロロ−２−イソプロピル−４−ペンテン酸エステルおよびその光学活性体の製造方法 |
| EP1626093A1 (en) * | 2004-08-11 | 2006-02-15 | Dow Global Technologies Inc. | Process for the production of (S)-5-chloro-2-isopropylpent-4-enoic acid esters |
| EP1856008A1 (en) * | 2005-03-09 | 2007-11-21 | DSM Fine Chemicals Austria Nfg GmbH & Co KG | Process for preparing enantiopure e-(2s)-alkyl-5-halopent-4-enoic acids and esters |
| JP4763771B2 (ja) * | 2005-03-17 | 2011-08-31 | ビーエーエスエフ ソシエタス・ヨーロピア | 光学活性３−フェニルプロピオン酸誘導体を生成する方法、およびその誘導体の後続生成物 |
| WO2006117057A1 (en) * | 2005-05-02 | 2006-11-09 | Dsm Fine Chemicals Austria Nfg Gmbh & Co Kg | Process for preparing enantiomerically enriched e-(2s)- and (2r)-alkyl-5-halopent-4-enecarboxylic acids or their esters |
| AT502257B1 (de) * | 2005-07-25 | 2007-04-15 | Dsm Fine Chem Austria Gmbh | Verfahren zur herstellung von racemischen alkyl-5-halogen-pent-4-en-carbonsäuren bzw. -carbonsäureestern |
| DE102005042458A1 (de) * | 2005-09-06 | 2007-03-22 | Basf Ag | Verfahren zur Herstellung von 2-substituierten Carbonsäuren |
| WO2007036491A1 (de) * | 2005-09-30 | 2007-04-05 | Basf Aktiengesellschaft | Verfahren zur herstellung von alpha-substituierten carbonsäuren |
| GB0521083D0 (en) | 2005-10-17 | 2005-11-23 | Novartis Ag | Organic compounds |
| GB2431654A (en) * | 2005-10-25 | 2007-05-02 | Novartis Ag | Alternative synthesis of aryl-octanoyl amide compounds |
| GB2431640A (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 |
| CA2631409C (en) * | 2005-12-16 | 2014-11-18 | Asahi Glass Company, Limited | Method for producing optically active (4e)-5-chloro-2-isopropyl-4-pentenoic acid or basic amino acid salt thereof |
| TW200837046A (en) * | 2006-11-08 | 2008-09-16 | Speedel Experimenta Ag | Process for preparing organic compounds |
| 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 |
| EP2062874B1 (en) | 2007-11-20 | 2014-12-17 | KRKA, tovarna zdravil, d.d., Novo mesto | Process and intermediates for the preparation of aliskiren |
| WO2009080773A1 (en) * | 2007-12-24 | 2009-07-02 | Dsm Ip Assets B.V. | Convergent synthesis of renin inhibitors and intermediates useful therein |
| EP2280937A1 (en) * | 2008-05-23 | 2011-02-09 | Teva Pharmaceutical Industries Ltd. | Aliskiren monofumarate and processes for preparation thereof |
| SI2189442T1 (sl) | 2008-11-20 | 2015-03-31 | Krka, Tovarna Zdravil, D.D., Novo Mesto | Postopek in intermediati za pripravo aliskirena |
| EP2393489B1 (en) | 2009-02-05 | 2014-10-08 | Krka, tovarna zdravil, d.d., Novo mesto | Moisture-activated granulation process |
| US8203005B2 (en) | 2009-10-29 | 2012-06-19 | Carbo Design Llc | Manufacturing process for enantiomerically pure 8-aryloctanoic acids as Aliskiren |
| CN101774986B (zh) | 2010-01-06 | 2012-03-28 | 浙江天宇药业股份有限公司 | 一种制备阿利克伦及其中间体的方法 |
| TR201002256A1 (tr) | 2010-03-24 | 2011-10-21 | Sanovel �La� Sanay� Ve T�Caret Anon�M ��Rket� | Stabil aliskiren formülasyonları |
| US20110268797A1 (en) | 2010-04-30 | 2011-11-03 | Sanovel IIac Sanayi Ve Ticaret Anonim Sirketi | Multicoated aliskiren formulations |
| SI2630118T1 (sl) | 2010-10-19 | 2015-03-31 | Mylan Laboratories Limited | Sinteza aliskirena |
| 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 |
| WO2013121443A1 (en) | 2012-02-17 | 2013-08-22 | Mylan Laboratories Ltd. | An improved 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 |
| CN103130677B (zh) * | 2013-03-12 | 2015-01-07 | 博瑞生物医药技术(苏州)有限公司 | 一种阿利克仑的制备方法 |
| AU2014300955B2 (en) * | 2013-06-27 | 2019-08-22 | Patheon Austria Gmbh & Co Kg | Preparation of Grignard reagents using a fluidized bed |
| CN103351300A (zh) * | 2013-06-30 | 2013-10-16 | 北京万全德众医药生物技术有限公司 | 一种制备阿利克仑中间体侧链（s）-2-溴代异戊酸甲酯的方法 |
| CN105294478B (zh) * | 2014-07-01 | 2017-06-13 | 华润双鹤药业股份有限公司 | 阿利吉仑的一种非对映异构体、其制备方法及用途 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4291057A (en) * | 1979-07-02 | 1981-09-22 | Union Carbide Corporation | Biocidal esters of halo-4-alkenoic acids |
| US4492799A (en) * | 1979-07-02 | 1985-01-08 | Union Carbide Corporation | Halo-4-alkenoic acids and their use as pesticidal intermediates |
| 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 |
| CA2247580A1 (en) * | 1997-10-03 | 1999-04-03 | F. Hoffmann-La Roche Ag | Process for preparing chiral succinic acid derivatives |
-
2000
- 2000-07-13 DE DE50006271T patent/DE50006271D1/de not_active Expired - Lifetime
- 2000-07-13 DK DK00940108T patent/DK1200390T3/da active
- 2000-07-13 DK DK00940109T patent/DK1200384T3/da active
- 2000-07-13 EP EP00940109A patent/EP1200384B1/de not_active Expired - Lifetime
- 2000-07-13 WO PCT/CH2000/000384 patent/WO2001009083A1/de not_active Ceased
- 2000-07-13 AT AT00940109T patent/ATE265415T1/de active
- 2000-07-13 JP JP2001514283A patent/JP4580606B2/ja not_active Expired - Lifetime
- 2000-07-13 AU AU55185/00A patent/AU5518500A/en not_active Abandoned
- 2000-07-13 JP JP2001514287A patent/JP4922521B2/ja not_active Expired - Fee Related
- 2000-07-13 DE DE50015330T patent/DE50015330D1/de not_active Expired - Lifetime
- 2000-07-13 EP EP00940108A patent/EP1200390B1/de not_active Expired - Lifetime
- 2000-07-13 WO PCT/CH2000/000385 patent/WO2001009079A1/de not_active Ceased
- 2000-07-13 AT AT00940108T patent/ATE406346T1/de active
- 2000-07-13 US US10/048,290 patent/US6777574B1/en not_active Expired - Fee Related
- 2000-07-13 ES ES00940108T patent/ES2312346T3/es not_active Expired - Lifetime
- 2000-07-13 US US10/048,229 patent/US7009078B1/en not_active Expired - Fee Related
- 2000-07-13 ES ES00940109T patent/ES2218173T3/es not_active Expired - Lifetime
- 2000-07-13 AU AU55184/00A patent/AU5518400A/en not_active Abandoned
- 2000-07-13 PT PT00940108T patent/PT1200390E/pt unknown
- 2000-07-13 PT PT00940109T patent/PT1200384E/pt unknown
-
2005
- 2005-10-21 US US11/254,749 patent/US7132569B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| WO2001009079A1 (de) | 2001-02-08 |
| ATE265415T1 (de) | 2004-05-15 |
| JP2003506345A (ja) | 2003-02-18 |
| US7009078B1 (en) | 2006-03-07 |
| PT1200390E (pt) | 2008-12-05 |
| US20060041169A1 (en) | 2006-02-23 |
| DE50006271D1 (de) | 2004-06-03 |
| DE50015330D1 (de) | 2008-10-09 |
| JP2003506347A (ja) | 2003-02-18 |
| US7132569B2 (en) | 2006-11-07 |
| US6777574B1 (en) | 2004-08-17 |
| EP1200390B1 (de) | 2008-08-27 |
| WO2001009083A1 (de) | 2001-02-08 |
| AU5518400A (en) | 2001-02-19 |
| PT1200384E (pt) | 2004-09-30 |
| DK1200390T3 (da) | 2008-12-01 |
| EP1200390A1 (de) | 2002-05-02 |
| ES2218173T3 (es) | 2004-11-16 |
| JP4580606B2 (ja) | 2010-11-17 |
| ES2312346T3 (es) | 2009-03-01 |
| EP1200384A1 (de) | 2002-05-02 |
| DK1200384T3 (da) | 2004-08-02 |
| EP1200384B1 (de) | 2004-04-28 |
| AU5518500A (en) | 2001-02-19 |
| JP4922521B2 (ja) | 2012-04-25 |
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