AR049283A1 - Procedimiento para la preparacion de derivados de difenil-azetidinona - Google Patents
Procedimiento para la preparacion de derivados de difenil-azetidinonaInfo
- Publication number
- AR049283A1 AR049283A1 ARP050102100A ARP050102100A AR049283A1 AR 049283 A1 AR049283 A1 AR 049283A1 AR P050102100 A ARP050102100 A AR P050102100A AR P050102100 A ARP050102100 A AR P050102100A AR 049283 A1 AR049283 A1 AR 049283A1
- Authority
- AR
- Argentina
- Prior art keywords
- general formula
- alkyl
- ch2n
- aryl
- compounds
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
- C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D205/06—Heterocyclic compounds containing four-membered rings with one nitrogen 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
- C07D205/08—Heterocyclic compounds containing four-membered rings with one nitrogen 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 one oxygen atom directly attached in position 2, e.g. beta-lactams
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Vascular Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Reivindicacion 1: Procedimiento para la preparacion de derivados de difenil-azetidinona de la formula general (1), o de las formas protegidas en los sustituyentes X, R1 y/o R2, en la que los símbolos, sustituyentes e índices tienen los siguientes significados, X = H, OH; R1 = OH, OCH3; R2 = F, CH2CH3, CH2NHR4; R3 = H, F; R4 = H, CO-(CH2-)nCO-R5, CO-(CH2-)nNHR6; n = numeros enteros de 4 a 16; R5 = OH, NH-CH2-[CH(OH)-]mCH2OH; R6 =H, CO-[CH(OH)-]mCH2OH; m = numeros enteros de 1 a 5, caracterizado porque compuestos de la formula general (2) con el significado de Y = H, H; H, OH; H, OAc; H, OSi(alquil)o(arilo)p, con o, p = 0, 1, 2 o 3 y o + p = 3; H, OTHP (THP significa el grupo protector tetrahidropiranilo); H, OC(arilo)3; H, OCH2Oalquilo; H, OCH(Oalquil)CH3; H, Oalquilo; H, OCH2arilo; Oalquilo, Oalquilo; un cetal cíclico tal como O-(CH2-)q-O con q = 2 o 3 se hacen reaccionar con iminas de la formula general (3) en que R7 = R1 y adicionalmente O-grupo protector; R8 = R2, CH2N[Si(alquil)o(aril)p]CO2CH2(C6H5), CH2N[Si(alquil)o(aril)p]CO2terbutilo, CH2N-CH(C6H5), CH2N=CH(C6H4-pOCH3), CH2N=CH[C6H4(R4)] y un resto de formula (4) resultando productos intermedios de la formula general (5), después de lo cual estas amino- amidas de la formula general (5) se transforman eventualmente en ésteres, anhídridos mixtos o ésteres activos de la formula general (6) pudiendo resultar entretanto la etapa del ácido carboxílico con R9 = H, y significando R9 = alquilo C1-4, CO- alquilo C1-4, COO-alquilo C1-4, SO2-arilo, y después de lo cual, a continuacion, los compuestos de la formula general (5) o eventualmente (6) se ciclizan para dar la lactama de la formula general (7), y eventualmente al final los compuestos de la formula general (7) se desprotegen y/o se hacen reaccionar en forma de aminas de la formula general (7), en las que R8, después de la desproteccion, significa R2, y ciertamente CH2NHR4 con R4 = H, con compuestos de las formulas generales (8) o (9) para dar los compuestos de la formula general (1).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102004025072A DE102004025072A1 (de) | 2004-05-21 | 2004-05-21 | Verfahren zur Herstellung von Diphenyl-azetidinon-Derivaten |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR049283A1 true AR049283A1 (es) | 2006-07-12 |
Family
ID=34968088
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050102100A AR049283A1 (es) | 2004-05-21 | 2005-05-20 | Procedimiento para la preparacion de derivados de difenil-azetidinona |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US7563888B2 (es) |
| EP (1) | EP1753717A1 (es) |
| JP (1) | JP2007538041A (es) |
| CN (1) | CN100582092C (es) |
| AR (1) | AR049283A1 (es) |
| AU (1) | AU2005245123A1 (es) |
| CA (1) | CA2567481A1 (es) |
| DE (1) | DE102004025072A1 (es) |
| IL (1) | IL178993A0 (es) |
| MX (1) | MXPA06013258A (es) |
| TW (1) | TW200611895A (es) |
| UY (1) | UY28913A1 (es) |
| WO (1) | WO2005113495A1 (es) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2002216097B2 (en) * | 2000-12-21 | 2006-09-07 | Sanofi-Aventis Deutschland Gmbh | Novel 1,2-diphenzylazetidinones, method for producing the same, medicaments containing said compounds, and the use thereof for treating disorders of the lipid metabolism |
| GB0215579D0 (en) | 2002-07-05 | 2002-08-14 | Astrazeneca Ab | Chemical compounds |
| BRPI0418004A (pt) | 2003-12-23 | 2007-04-17 | Astrazeneca Ab | composto ou um sal, solvato, solvato de um tal sal ou uma pró-droga deste farmaceuticamente aceitáveis, métodos para tratar ou prevenir condições hiperlipidêmicas, aterosclerose, mal de alzheimer, e tumores associados com colesterol, formulação farmacêutica, combinação, e, processo para preparar um composto ou um sal, solvato, solvato de um tal sal ou uma pró-droga deste farmaceuticamente aceitáveis |
| UY29607A1 (es) | 2005-06-20 | 2007-01-31 | Astrazeneca Ab | Compuestos quimicos |
| SA06270191B1 (ar) | 2005-06-22 | 2010-03-29 | استرازينيكا ايه بي | مشتقات من 2- أزيتيدينون جديدة باعتبارها مثبطات لامتصاص الكوليسترول لعلاج حالات فرط نسبة الدهون في الدم |
| AR057072A1 (es) | 2005-06-22 | 2007-11-14 | Astrazeneca Ab | Compuestos quimicos derivados de 2-azetidinona, formulacion farmaceutica y un proceso de preparacion del compuesto |
| AR060623A1 (es) | 2006-04-27 | 2008-07-02 | Astrazeneca Ab | Compuestos derivados de 2-azetidinona y un metodo de preparacion |
| JP5059355B2 (ja) * | 2006-08-01 | 2012-10-24 | 壽製薬株式会社 | オキサゾリジン誘導体の製造方法 |
| CZ302395B6 (cs) * | 2007-03-02 | 2011-04-27 | Zentiva, A. S. | Zpusob výroby (3R,4S)-1-(4-fluorfenyl)-3-[(3S)-3-(4-fluorfenyl)-3-hydroxypropyl)]-4-(4-hydroxyfenyl)-2-azetidinonu |
| WO2008108486A1 (ja) | 2007-03-06 | 2008-09-12 | Teijin Pharma Limited | １－ビアリールアゼチジノン誘導体 |
| US20090047716A1 (en) * | 2007-06-07 | 2009-02-19 | Nurit Perlman | Reduction processes for the preparation of ezetimibe |
| DE102007063671A1 (de) * | 2007-11-13 | 2009-06-25 | Sanofi-Aventis Deutschland Gmbh | Neue kristalline Diphenylazetidinonhydrate, diese Verbindungen enthaltende Arzneimittel und deren Verwendung |
| WO2010113175A2 (en) | 2009-04-01 | 2010-10-07 | Matrix Laboratories Ltd | Enzymatic process for the preparation of (s)-5-(4-fluoro-phenyl)-5-hydroxy- 1morpholin-4-yl-pentan-1-one, an intermediate of ezetimibe and further conversion to ezetimibe |
| WO2015039675A1 (en) | 2013-09-23 | 2015-03-26 | Pharmathen S.A. | Novel process for the preparation of ezetimibe intermediates |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUT67341A (en) * | 1991-07-23 | 1995-03-28 | Schering Corp | Substituted beta-lactam compounds useful as hypocholesterolemic agents, pharmaceutical compositions containing the same and process for the production thereof |
-
2004
- 2004-05-21 DE DE102004025072A patent/DE102004025072A1/de not_active Withdrawn
-
2005
- 2005-05-20 AU AU2005245123A patent/AU2005245123A1/en not_active Abandoned
- 2005-05-20 UY UY28913A patent/UY28913A1/es unknown
- 2005-05-20 AR ARP050102100A patent/AR049283A1/es not_active Application Discontinuation
- 2005-05-20 EP EP05743217A patent/EP1753717A1/de not_active Withdrawn
- 2005-05-20 CA CA002567481A patent/CA2567481A1/en not_active Abandoned
- 2005-05-20 CN CN200580016190A patent/CN100582092C/zh not_active Expired - Fee Related
- 2005-05-20 TW TW094116388A patent/TW200611895A/zh unknown
- 2005-05-20 MX MXPA06013258A patent/MXPA06013258A/es active IP Right Grant
- 2005-05-20 JP JP2007517093A patent/JP2007538041A/ja not_active Abandoned
- 2005-05-20 WO PCT/EP2005/005497 patent/WO2005113495A1/de not_active Application Discontinuation
-
2006
- 2006-11-01 IL IL178993A patent/IL178993A0/en unknown
- 2006-11-07 US US11/557,310 patent/US7563888B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| IL178993A0 (en) | 2007-03-08 |
| EP1753717A1 (de) | 2007-02-21 |
| WO2005113495A1 (de) | 2005-12-01 |
| JP2007538041A (ja) | 2007-12-27 |
| UY28913A1 (es) | 2005-12-30 |
| CN100582092C (zh) | 2010-01-20 |
| CN1956951A (zh) | 2007-05-02 |
| TW200611895A (en) | 2006-04-16 |
| US20070149501A1 (en) | 2007-06-28 |
| CA2567481A1 (en) | 2005-12-01 |
| MXPA06013258A (es) | 2007-02-28 |
| US7563888B2 (en) | 2009-07-21 |
| DE102004025072A1 (de) | 2005-12-15 |
| AU2005245123A1 (en) | 2005-12-01 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |