ATE340159T1 - Verfahren zur herstellung von alfentanil, sufentanil und remifentanil - Google Patents

Verfahren zur herstellung von alfentanil, sufentanil und remifentanil

Info

Publication number
ATE340159T1
ATE340159T1 AT00988013T AT00988013T ATE340159T1 AT E340159 T1 ATE340159 T1 AT E340159T1 AT 00988013 T AT00988013 T AT 00988013T AT 00988013 T AT00988013 T AT 00988013T AT E340159 T1 ATE340159 T1 AT E340159T1
Authority
AT
Austria
Prior art keywords
remifentanil
alfentanil
sufentanil
producing
synthesizing
Prior art date
Application number
AT00988013T
Other languages
English (en)
Inventor
Jacob Mathew
J Kendall Killgore
Original Assignee
Mallinckrodt Inc
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 Mallinckrodt Inc filed Critical Mallinckrodt Inc
Application granted granted Critical
Publication of ATE340159T1 publication Critical patent/ATE340159T1/de

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/56Nitrogen atoms
    • C07D211/58Nitrogen atoms attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • C07D211/66Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4 having a hetero atom as the second substituent in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
AT00988013T 1999-12-06 2000-12-04 Verfahren zur herstellung von alfentanil, sufentanil und remifentanil ATE340159T1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US16873999P 1999-12-06 1999-12-06

Publications (1)

Publication Number Publication Date
ATE340159T1 true ATE340159T1 (de) 2006-10-15

Family

ID=22612741

Family Applications (1)

Application Number Title Priority Date Filing Date
AT00988013T ATE340159T1 (de) 1999-12-06 2000-12-04 Verfahren zur herstellung von alfentanil, sufentanil und remifentanil

Country Status (10)

Country Link
US (2) US7074935B2 (de)
EP (1) EP1246801B1 (de)
JP (1) JP2003515588A (de)
AT (1) ATE340159T1 (de)
AU (1) AU2427201A (de)
BR (1) BR0016063A (de)
CA (1) CA2393559C (de)
DE (1) DE60030883T2 (de)
ES (1) ES2272354T3 (de)
WO (1) WO2001040184A2 (de)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10141650C1 (de) 2001-08-24 2002-11-28 Lohmann Therapie Syst Lts Transdermales Therapeutisches System mit Fentanyl bzw. verwandten Substanzen
AU2004287815B2 (en) * 2003-10-29 2009-05-28 Mallinckrodt Inc. Industrial method for separation and purification of fentanyl by reverse phase preparative chromatography
JP2008519837A (ja) * 2004-11-10 2008-06-12 ベーリンガー インゲルハイム ケミカルズ インコーポレイテッド フェンタニル中間体の生成方法
GB0509276D0 (en) * 2005-05-06 2005-06-15 Univ Cranfield Synthetic receptor
CN101312949A (zh) * 2005-11-17 2008-11-26 马林克罗特公司 合成瑞芬太尼的方法
US8252328B2 (en) * 2006-01-06 2012-08-28 Acelrx Pharmaceuticals, Inc. Bioadhesive drug formulations for oral transmucosal delivery
US8357114B2 (en) 2006-01-06 2013-01-22 Acelrx Pharmaceuticals, Inc. Drug dispensing device with flexible push rod
US8865743B2 (en) 2006-01-06 2014-10-21 Acelrx Pharmaceuticals, Inc. Small volume oral transmucosal dosage forms containing sufentanil for treatment of pain
US8753308B2 (en) 2006-01-06 2014-06-17 Acelrx Pharmaceuticals, Inc. Methods for administering small volume oral transmucosal dosage forms using a dispensing device
US8535714B2 (en) 2006-01-06 2013-09-17 Acelrx Pharmaceuticals, Inc. Small volume oral transmucosal dosage forms containing sufentanil for treatment of pain
US8202535B2 (en) 2006-01-06 2012-06-19 Acelrx Pharmaceuticals, Inc. Small-volume oral transmucosal dosage forms
US9289583B2 (en) 2006-01-06 2016-03-22 Acelrx Pharmaceuticals, Inc. Methods for administering small volume oral transmucosal dosage forms using a dispensing device
US8252329B2 (en) 2007-01-05 2012-08-28 Acelrx Pharmaceuticals, Inc. Bioadhesive drug formulations for oral transmucosal delivery
US9066847B2 (en) * 2007-01-05 2015-06-30 Aceirx Pharmaceuticals, Inc. Storage and dispensing devices for administration of oral transmucosal dosage forms
JP2009525329A (ja) * 2006-02-03 2009-07-09 マリンクロッド・インコーポレイテッド レミフェンタニル塩酸塩の結晶形
US20070260491A1 (en) * 2006-05-08 2007-11-08 Pamela Palmer System for delivery and monitoring of administration of controlled substances
EP1867635A1 (de) * 2006-06-15 2007-12-19 Kern Pharma, S.L. Verfahren zur Herstellung von Remifentanil, seine Zwischenprodukte, die Verwendung von diesen Zwischenprodukten und das Verfahren zur deren Herstellung
US20070299687A1 (en) * 2006-06-23 2007-12-27 Pamela Palmer Inpatient system for patient-controlled delivery of oral transmucosal medications dosed as needed
WO2008045192A2 (en) * 2006-10-05 2008-04-17 Mallinckrodt Inc. Alternate process for remifentanil preparation
CA2670704A1 (en) * 2006-11-29 2008-06-05 Mallinckrodt Inc. New process for remifentanil synthesis
JP2011526257A (ja) * 2008-07-03 2011-10-06 シラグ アーゲー N−フェニル−n−(4−ピペリジニル)アミド塩の製造方法
WO2010027770A1 (en) * 2008-09-04 2010-03-11 Mallinckrodt Inc. Crystalline forms of sufentanil citrate
US8299258B2 (en) 2008-11-04 2012-10-30 Cambrex Charles City Method of making piperidine derivatives
US8945592B2 (en) * 2008-11-21 2015-02-03 Acelrx Pharmaceuticals, Inc. Sufentanil solid dosage forms comprising oxygen scavengers and methods of using the same
ES2664801T3 (es) * 2010-09-17 2018-04-23 Mallinckrodt Llc Proceso mejorado para la preparación de un precursor de sufentanilo base
EP2455377B1 (de) 2010-11-11 2014-07-09 hameln rds gmbh Synthese von Fentanyl Analoga
CN102060753B (zh) * 2010-12-29 2013-01-09 宜昌人福药业有限责任公司 一种4-苯胺基哌啶类镇痛药的精制方法
CN103044398B (zh) * 2012-12-12 2015-09-16 宜昌人福药业有限责任公司 一种盐酸阿芬太尼的晶型
US8742111B1 (en) * 2013-02-21 2014-06-03 The United States Of America As Represented By The Secretary Of The Army Synthesis of intermediate anilino methyl esters used in the production of synthetic opioid analgesics
EP3183232B1 (de) * 2014-08-22 2023-05-03 The Arizona Board of Regents on behalf of The University of Arizona Substituierte 1-arylethyl-4-acylaminopiperidin-derivate als opioid-/alpha-adrenorezeptor-modulatoren und verfahren zu deren herstellung
EP3233799B1 (de) 2014-12-19 2021-05-19 The Broad Institute, Inc. Dopamin-d2-rezeptor-liganden
EP3233077A4 (de) 2014-12-19 2018-08-08 The Broad Institute Inc. Dopamin-d2-rezeptor-liganden
ES2806631T3 (es) 2015-05-27 2021-02-18 SpecGx LLC Preparación de citrato de sufentanilo y base de sufentanilo
SI3199523T1 (sl) 2016-01-29 2018-12-31 Bioka S.R.O. Nov postopek za pridobivanje n-fenil-n-(4-piperinidil)amidnih derivatov kot sta remifentanil in karfentanil
WO2017180659A1 (en) * 2016-04-11 2017-10-19 Arizona Board Of Regents On Behalf Of University Of Arizona Opioid receptor modulators
US9650338B1 (en) 2016-07-29 2017-05-16 VDM Biochemicals, Inc. Opioid antagonist compounds and methods of making and using
WO2022195497A1 (en) * 2021-03-16 2022-09-22 Ami Organics Ltd. A process for the preparation of 4-piperidone hcl hydrate

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3161644A (en) 1962-06-22 1964-12-15 Res Lab Dr C Janssen N V 1-benzyl-4-substituted piperidines
US3998834A (en) * 1975-03-14 1976-12-21 Janssen Pharmaceutica N.V. N-(4-piperidinyl)-n-phenylamides and -carbamates
FR2389622B1 (de) * 1977-05-05 1982-05-21 Janssen Pharmaceutica Nv
US4167574A (en) 1978-03-13 1979-09-11 Janssen Pharmaceutica, N.V. N-phenyl-N-(4-piperidinyl)amides
US5019583A (en) 1989-02-15 1991-05-28 Glaxo Inc. N-phenyl-N-(4-piperidinyl)amides useful as analgesics
US5461147A (en) 1993-09-27 1995-10-24 Schering Corporation Process for preparing benzazepine intermediates for the synthesis of D1 antagonists
US5489689A (en) 1993-09-30 1996-02-06 Mallinckrodt Chemical, Inc. Preparation of piperidine derivatives

Also Published As

Publication number Publication date
US20040138461A1 (en) 2004-07-15
US7208604B2 (en) 2007-04-24
AU2427201A (en) 2001-06-12
US20060149071A1 (en) 2006-07-06
EP1246801B1 (de) 2006-09-20
CA2393559C (en) 2009-05-26
DE60030883D1 (de) 2006-11-02
ES2272354T3 (es) 2007-05-01
WO2001040184B1 (en) 2002-01-31
DE60030883T2 (de) 2007-09-06
BR0016063A (pt) 2002-08-06
EP1246801A2 (de) 2002-10-09
CA2393559A1 (en) 2001-06-07
US7074935B2 (en) 2006-07-11
JP2003515588A (ja) 2003-05-07
WO2001040184A3 (en) 2002-01-03
WO2001040184A2 (en) 2001-06-07

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