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AR054374A1 - Procedimientos utiles para sintesis de compuestos farmaceuticos en especial inhibidores de renina (aliskiren), intermediarios y compuestos farmaceuticos - Google Patents

Procedimientos utiles para sintesis de compuestos farmaceuticos en especial inhibidores de renina (aliskiren), intermediarios y compuestos farmaceuticos

Info

Publication number
AR054374A1
AR054374A1 ARP060102357A ARP060102357A AR054374A1 AR 054374 A1 AR054374 A1 AR 054374A1 AR P060102357 A ARP060102357 A AR P060102357A AR P060102357 A ARP060102357 A AR P060102357A AR 054374 A1 AR054374 A1 AR 054374A1
Authority
AR
Argentina
Prior art keywords
formula
compound
salt
manufacture
pharmaceutical compounds
Prior art date
Application number
ARP060102357A
Other languages
English (en)
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR054374A1 publication Critical patent/AR054374A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/22Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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 no double bonds between ring members or between ring members and non-ring members
    • C07D207/08Heterocyclic 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 no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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 no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic 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 no 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
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/26Heterocyclic 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
    • C07D307/30Heterocyclic 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
    • C07D307/32Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/26Heterocyclic 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
    • C07D307/30Heterocyclic 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
    • C07D307/32Oxygen atoms
    • C07D307/33Oxygen atoms in position 2, the oxygen atom being in its keto or unsubstituted enol form
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design 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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Furan Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

La presente se refiere a procedimientos, compuestos e intermediarios utiles en la síntesis de compuestos farmacéuticamente activos, en especial inhibidores de renina, tales como aliskiren. Reivindicacion 1: un procedimiento para la fabricacion de un compuesto de la formula (3) en donde R es H, alquilo o alcoxialquilo; R1 es H, alquilo o alcoxialquilo; R2 es H o de preferencia un grupo hidroxilo-protector; R3 es H o alquilo no sustituido o sustituido; y PG es un grupo amino-protector, especialmente uno que se puede remover a través de hidrolisis, por ejemplo alcoxicarbonilo inferior, tal como ter-butoxicarbonilo o benciloxicarbonilo; o una sal del mismo; dicho procedimiento comprende hacer reaccionar un compuesto en la formula (1) en donde R, R1, R2, R3 y PG son como se definieron para un compuesto de la formula (3), con u residuo capaz de transformar el hidroxi en la formula I a X, en donde X es un grupo distinto a hidroxi o H, especialmente un grupo saliente, en especial un reactor seleccionado de ácido hidrohálico, una halogenuro de tionilo, PX*3, POX*3, PX*5 o POX*5 en donde X* es un halogenuro, una combinacion de trifenilfosfina y halogeno, y un derivado activo de un ácido sulfonico orgánico. Reivindicacion 61: La fabricacion de un compuesto de la formula (15), en donde R, R1, y PG son como se definieron para un compuesto de la formula (3) en cualquiera de las reivindicaciones 1 a 3 o como se da en la reivindicacion 4, o una sal del mismo, que comprende uno o más, por ejemplo todos los pasos de: (i) la fabricacion de un compuesto de la formula (3) de acuerdo con cualquiera de las reivindicaciones 1 a 3, o una sal del mismo, la fabricacion de un compuesto de la formula (4) de acuerdo con a reivindicacion 5, o una sal del mismo, o (ii) la fabricacion de un compuesto de la formula (4S) de acuerdo con la reivindicacion 8, o una sal del mismo, la fabricacion de un compuesto de la formula (4) de acuerdo con la reivindicacion 9, o una sal del mismo, la fabricacion de un compuesto de la formula (5) o una sal del mismo, de acuerdo con la reivindicacion 10, la fabricacion de un compuesto de la formula (23) o una sal del mismo, de acuerdo con la reivindicacion 56, la fabricacion de un compuesto de la formula (24) o una sal del mismo, de acuerdo con la reivindicacion 58, la fabricacion de un compuesto de la formula (20), o una sal del mismo, de acuerdo con la reivindicacion 60, la fabricacion de un compuesto de la formula (14) o una sal del mismo, de acuerdo con la reivindicacion 47, y la desproteccion del mismo de acuerdo con la reivindicacion 33 a un compuesto de la formula (15), o una sal del mismo, y si se desea, convertir un compuesto libre obtenible de la formula (15) a una sal, o una sal obtenible al compuesto libre de la formula (15) o una sal diferente del mismo.
ARP060102357A 2005-06-08 2006-06-06 Procedimientos utiles para sintesis de compuestos farmaceuticos en especial inhibidores de renina (aliskiren), intermediarios y compuestos farmaceuticos AR054374A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0511686.8A GB0511686D0 (en) 2005-06-08 2005-06-08 Organic compounds

Publications (1)

Publication Number Publication Date
AR054374A1 true AR054374A1 (es) 2007-06-20

Family

ID=34835327

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060102357A AR054374A1 (es) 2005-06-08 2006-06-06 Procedimientos utiles para sintesis de compuestos farmaceuticos en especial inhibidores de renina (aliskiren), intermediarios y compuestos farmaceuticos

Country Status (24)

Country Link
US (2) US7767831B2 (es)
EP (2) EP2080754A3 (es)
JP (2) JP2008542415A (es)
KR (1) KR20080014011A (es)
CN (1) CN101193860B (es)
AR (1) AR054374A1 (es)
AU (1) AU2006256938B2 (es)
BR (1) BRPI0611919A2 (es)
CA (1) CA2608575A1 (es)
EC (1) ECSP077986A (es)
GB (1) GB0511686D0 (es)
GT (1) GT200600208A (es)
IL (1) IL187004A0 (es)
MA (1) MA29563B1 (es)
MX (1) MX2007015418A (es)
NO (1) NO20080080L (es)
NZ (2) NZ562889A (es)
PE (2) PE20070075A1 (es)
RU (1) RU2418785C2 (es)
SG (1) SG155209A1 (es)
TN (1) TNSN07465A1 (es)
TW (1) TW200716544A (es)
WO (1) WO2006131304A2 (es)
ZA (1) ZA200709076B (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0521083D0 (en) 2005-10-17 2005-11-23 Novartis Ag Organic 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
EP2225200B1 (en) 2007-12-24 2013-10-16 DSM IP Assets B.V. Convergent synthesis of renin inhibitors and intermediates useful therein
SI2189442T1 (sl) 2008-11-20 2015-03-31 Krka, Tovarna Zdravil, D.D., Novo Mesto Postopek in intermediati za pripravo aliskirena
EP2464623B1 (en) 2009-08-11 2020-11-04 Novartis AG The ring opening of lactones and lactams
US8203005B2 (en) 2009-10-29 2012-06-19 Carbo Design Llc Manufacturing process for enantiomerically pure 8-aryloctanoic acids as Aliskiren
EP2523934A1 (en) * 2010-02-10 2012-11-21 Ratiopharm GmbH Salts of aliskiren
US8703976B2 (en) 2011-10-02 2014-04-22 Milan Soukup Manufacturing process for 8-aryloctanoic acids such as Aliskiren
CN111423325A (zh) * 2020-04-26 2020-07-17 江苏凯迪恩医药科技有限公司 基于蒽醌类药物的双醋瑞因合成方法

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4570108A (en) * 1982-07-06 1986-02-11 Stroede Aake Protection device for electrical incandescent lamps
US5659065A (en) 1994-04-18 1997-08-19 Novartis Corporation Alpha-aminoalkanoic acids and reduction products
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
CA2121898A1 (en) * 1994-04-21 1995-10-22 Stephen Hanessian Synthesis of prototypes for renin inhibitors
IT1292426B1 (it) * 1997-06-27 1999-02-08 Nicox Sa Sali nitrati di ace-inibitori
JP2005231999A (ja) * 2000-03-08 2005-09-02 Banyu Pharmaceut Co Ltd カルバペネム誘導体の製造方法
PL212898B1 (pl) 2000-07-05 2012-12-31 Speedel Pharma Ag Sposób otrzymywania podstawionych amidów oktanoilowych oraz zwiazki posrednie wykorzystane w tym sposobie
US8168616B1 (en) * 2000-11-17 2012-05-01 Novartis Ag Combination comprising a renin inhibitor and an angiotensin receptor inhibitor for hypertension
ATE342887T1 (de) * 2000-12-14 2006-11-15 Speedel Pharma Ag Verfahren zur herstellung von aryloctanoyl-amiden
GB0419361D0 (en) 2004-08-31 2004-10-06 Novartis Ag Organic compounds

Also Published As

Publication number Publication date
ZA200709076B (en) 2008-10-29
WO2006131304A2 (en) 2006-12-14
IL187004A0 (en) 2008-02-09
CA2608575A1 (en) 2006-12-14
PE20070075A1 (es) 2007-03-16
WO2006131304A3 (en) 2007-07-19
NO20080080L (no) 2008-01-04
CN101193860B (zh) 2013-01-02
KR20080014011A (ko) 2008-02-13
RU2418785C2 (ru) 2011-05-20
TW200716544A (en) 2007-05-01
NZ591010A (en) 2012-06-29
CN101193860A (zh) 2008-06-04
BRPI0611919A2 (pt) 2010-10-05
NZ562889A (en) 2011-11-25
JP2013028607A (ja) 2013-02-07
US7767831B2 (en) 2010-08-03
AU2006256938A1 (en) 2006-12-14
AU2006256938B2 (en) 2009-12-17
RU2007148226A (ru) 2009-07-20
EP2080754A3 (en) 2010-06-02
EP1896411A2 (en) 2008-03-12
JP2008542415A (ja) 2008-11-27
PE20091359A1 (es) 2009-10-13
US20100274027A1 (en) 2010-10-28
TNSN07465A1 (en) 2009-03-17
ECSP077986A (es) 2008-01-23
MX2007015418A (es) 2008-02-21
US20080207921A1 (en) 2008-08-28
GT200600208A (es) 2007-03-28
SG155209A1 (en) 2009-09-30
EP2080754A2 (en) 2009-07-22
GB0511686D0 (en) 2005-07-13
MA29563B1 (fr) 2008-06-02

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