DE60030883D1 - Verfahren zur herstellung von alfentanil, sufentanil und remifentanil - Google Patents

Verfahren zur herstellung von alfentanil, sufentanil und remifentanil

Info

Publication number
DE60030883D1
DE60030883D1 DE60030883T DE60030883T DE60030883D1 DE 60030883 D1 DE60030883 D1 DE 60030883D1 DE 60030883 T DE60030883 T DE 60030883T DE 60030883 T DE60030883 T DE 60030883T DE 60030883 D1 DE60030883 D1 DE 60030883D1
Authority
DE
Germany
Prior art keywords
remifentanil
alfentanil
sufentanil
preparation
synthesizing
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
DE60030883T
Other languages
English (en)
Other versions
DE60030883T2 (de
Inventor
Jacob Mathew
Kendall Killgore
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Mallinckrodt Inc
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 DE60030883D1 publication Critical patent/DE60030883D1/de
Publication of DE60030883T2 publication Critical patent/DE60030883T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/06—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic 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
    • C07D211/36—Heterocyclic 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
    • C07D211/56—Nitrogen atoms
    • C07D211/58—Nitrogen atoms attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic 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
    • C07D211/36—Heterocyclic 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon 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
    • C07D211/66—Carbon 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic 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)
DE60030883T 1999-12-06 2000-12-04 Verfahren zur herstellung von alfentanil, sufentanil und remifentanil Expired - Fee Related DE60030883T2 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US16873999P 1999-12-06 1999-12-06
PCT/US2000/032882 WO2001040184A2 (en) 1999-12-06 2000-12-04 Methods for the syntheses of alfentanil, sufentanil and remifentanil
US168739P 2009-04-13

Publications (2)

Publication Number Publication Date
DE60030883D1 true DE60030883D1 (de) 2006-11-02
DE60030883T2 DE60030883T2 (de) 2007-09-06

Family

ID=22612741

Family Applications (1)

Application Number Title Priority Date Filing Date
DE60030883T Expired - Fee Related DE60030883T2 (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
EP1682505B1 (de) * 2003-10-29 2008-12-24 Mallinckrodt Inc. Grosstechnisches verfahren zur abtrennung und aufreinigung von fentanyl durch präparative umkehrphasenchromatographie
WO2006055321A2 (en) * 2004-11-10 2006-05-26 Boehringer Ingelheim Chemicals, Inc. Process of making fentanyl intermediates
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
US8535714B2 (en) 2006-01-06 2013-09-17 Acelrx Pharmaceuticals, Inc. Small volume oral transmucosal dosage forms containing sufentanil for treatment of pain
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
US8753308B2 (en) 2006-01-06 2014-06-17 Acelrx Pharmaceuticals, Inc. Methods for administering small volume oral transmucosal dosage forms using a dispensing device
US8357114B2 (en) 2006-01-06 2013-01-22 Acelrx Pharmaceuticals, Inc. Drug dispensing device with flexible push rod
US9289583B2 (en) 2006-01-06 2016-03-22 Acelrx Pharmaceuticals, Inc. Methods for administering small volume oral transmucosal dosage forms using a dispensing device
US8865743B2 (en) 2006-01-06 2014-10-21 Acelrx Pharmaceuticals, Inc. Small volume oral transmucosal dosage forms containing sufentanil for treatment of pain
US8252328B2 (en) * 2006-01-06 2012-08-28 Acelrx Pharmaceuticals, Inc. Bioadhesive drug formulations for oral transmucosal delivery
US8202535B2 (en) * 2006-01-06 2012-06-19 Acelrx Pharmaceuticals, Inc. Small-volume oral transmucosal dosage forms
CA2641283A1 (en) * 2006-02-03 2007-08-16 Mallinckrodt Inc. Crystalline form of remifentanil hydrochloride
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
EP2081899A2 (de) * 2006-10-05 2009-07-29 Mallinckrodt Inc. Alternatives verfahren zur herstellung von remifentanil
CA2670704A1 (en) * 2006-11-29 2008-06-05 Mallinckrodt Inc. New process for remifentanil synthesis
US20110144346A1 (en) * 2008-07-03 2011-06-16 Cilag Ag Method for producing n-phenyl-n-(4-piperidinyl) amide salts
WO2010027770A1 (en) * 2008-09-04 2010-03-11 Mallinckrodt Inc. Crystalline forms of sufentanil citrate
WO2010053944A1 (en) * 2008-11-04 2010-05-14 Cambrex Charles City, Inc. Improved 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
WO2012037309A2 (en) * 2010-09-17 2012-03-22 Mallinckrodt Llc Improved process for the preparation of sufentanil base and related compounds
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
WO2016100940A1 (en) 2014-12-19 2016-06-23 The Broad Institute, Inc. Dopamine d2 receptor ligands
US10752588B2 (en) 2014-12-19 2020-08-25 The Broad Institute, Inc. Dopamine D2 receptor ligands
BR112017025115B1 (pt) 2015-05-27 2023-03-14 Mallinckrodt Llc Processo para formar citrato de sufentanila a partir de base de sufentanila
DK3199523T3 (en) 2016-01-29 2018-11-26 Bioka S R O NEW PROCEDURE FOR THE PREPARATION OF N-PHENYL-N- (4-PIPERIDINYL) AMIDE DERIVATIVES, SUCH AS REMIFENTANIL AND CARFENTANIL
US10766925B2 (en) * 2016-04-11 2020-09-08 Arizona Board Of Regents On Behalf Of The 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
EP1246801A2 (de) 2002-10-09
US20040138461A1 (en) 2004-07-15
DE60030883T2 (de) 2007-09-06
JP2003515588A (ja) 2003-05-07
AU2427201A (en) 2001-06-12
CA2393559C (en) 2009-05-26
US7208604B2 (en) 2007-04-24
EP1246801B1 (de) 2006-09-20
WO2001040184B1 (en) 2002-01-31
ES2272354T3 (es) 2007-05-01
WO2001040184A2 (en) 2001-06-07
US20060149071A1 (en) 2006-07-06
ATE340159T1 (de) 2006-10-15
WO2001040184A3 (en) 2002-01-03
US7074935B2 (en) 2006-07-11
BR0016063A (pt) 2002-08-06
CA2393559A1 (en) 2001-06-07

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Legal Events

Date Code Title Description
8364 No opposition during term of opposition
8339 Ceased/non-payment of the annual fee