SE9300013L - New procedure and intermediates for the manufacture of prodrugs - Google Patents

New procedure and intermediates for the manufacture of prodrugs

Info

Publication number
SE9300013L
SE9300013L SE9300013A SE9300013A SE9300013L SE 9300013 L SE9300013 L SE 9300013L SE 9300013 A SE9300013 A SE 9300013A SE 9300013 A SE9300013 A SE 9300013A SE 9300013 L SE9300013 L SE 9300013L
Authority
SE
Sweden
Prior art keywords
formula
salt
tranexamic acid
substituted
prodrug
Prior art date
Application number
SE9300013A
Other languages
Unknown language ( )
Swedish (sv)
Other versions
SE9300013D0 (en
Inventor
Nilsaake Joensson
Original Assignee
Kabi Pharmacia Ab
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 Kabi Pharmacia Ab filed Critical Kabi Pharmacia Ab
Priority to SE9300013A priority Critical patent/SE9300013L/en
Publication of SE9300013D0 publication Critical patent/SE9300013D0/en
Priority to PCT/SE1993/001115 priority patent/WO1994015904A1/en
Priority to AU58452/94A priority patent/AU5845294A/en
Publication of SE9300013L publication Critical patent/SE9300013L/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C251/00—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
    • C07C251/02—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton containing imino groups
    • C07C251/24—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton containing imino groups having carbon atoms of imino groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/14—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof
    • C07C227/18—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions involving amino or carboxyl groups, e.g. hydrolysis of esters or amides, by formation of halides, salts or esters
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/46—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

A tranexamic acid prodrug of general formula (II), is prepared by conversion of tranexamic acid in aqueous solution into a salt. An aromatic aldehyde of the formula Ar-CHO, lacking alpha -hydrogen atom is added to the solution and water is removed so as to form a salt of formula (a). The obtained suspension of anhydrous N-substituted tranexamic acid salt is esterified with 1-halogenethyl ethyl carbonate, wherein the halogen is chloro or bromo, and the halogenide formed and possibly present catalyst are removed. Protected esters of formula (b) wherein R signifies phenyl or naphthyl which may be substituted with lower alkyl or lower alkoxy groups or halogen atoms, are novel intermediates which can be used for the preparation of the prodrug (II).
SE9300013A 1992-12-30 1992-12-30 New procedure and intermediates for the manufacture of prodrugs SE9300013L (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
SE9300013A SE9300013L (en) 1992-12-30 1992-12-30 New procedure and intermediates for the manufacture of prodrugs
PCT/SE1993/001115 WO1994015904A1 (en) 1992-12-30 1993-12-30 Novel process and intermediates for the preparation of prodrugs
AU58452/94A AU5845294A (en) 1992-12-30 1993-12-30 Novel process and intermediates for the preparation of prodrugs

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
SE9300013A SE9300013L (en) 1992-12-30 1992-12-30 New procedure and intermediates for the manufacture of prodrugs

Publications (2)

Publication Number Publication Date
SE9300013D0 SE9300013D0 (en) 1992-12-30
SE9300013L true SE9300013L (en) 1994-07-01

Family

ID=20388467

Family Applications (1)

Application Number Title Priority Date Filing Date
SE9300013A SE9300013L (en) 1992-12-30 1992-12-30 New procedure and intermediates for the manufacture of prodrugs

Country Status (3)

Country Link
AU (1) AU5845294A (en)
SE (1) SE9300013L (en)
WO (1) WO1994015904A1 (en)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050025825A1 (en) 2003-07-31 2005-02-03 Xanodyne Pharmacal, Inc. Tranexamic acid formulations with reduced adverse effects
AU2004267100B2 (en) 2003-08-20 2010-10-07 Xenoport, Inc. Acyloxyalkyl carbamate prodrugs, methods of synthesis and use
ES2405329T3 (en) 2003-12-30 2013-05-30 Xenoport, Inc. Synthesis of acyloxyalkyl carbonate prodrugs and intermediates thereof
US20090215898A1 (en) 2004-03-04 2009-08-27 Xanodyne Pharmaceuticals, Inc. Tranexamic acid formulations
US8022106B2 (en) 2004-03-04 2011-09-20 Ferring B.V. Tranexamic acid formulations
US20050244495A1 (en) 2004-03-04 2005-11-03 Xanodyne Pharmaceuticals, Inc. Tranexamic acid formulations
US7947739B2 (en) 2004-03-04 2011-05-24 Ferring B.V. Tranexamic acid formulations
JP4938771B2 (en) 2005-06-20 2012-05-23 ゼノポート，インコーポレーテッド Acyloxyalkyl carbamate prodrugs of tranexamic acid, methods of synthesis, and uses
US20110060040A1 (en) 2009-09-04 2011-03-10 Xenoport, Inc. Uses of acyloxyalkyl carbamate prodrugs of tranexamic acid
WO2011091164A1 (en) 2010-01-22 2011-07-28 Xenoport, Inc. Oral dosage forms having a high loading of a tranexamic acid prodrug
CN116284814A (en) * 2023-01-17 2023-06-23 杭州三式化妆品有限公司 Supermolecule tranexamic acid glycolate ion salt and preparation method and application thereof

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4377594A (en) * 1980-06-04 1983-03-22 Kureha Kagaku Kogyo Kabushiki Kaisha Derivative of 4-(N-(substituted-benzylidene)amino-methyl cyclohexane-1-carboxylic acid
EP0079872B1 (en) * 1981-11-17 1985-03-20 KabiVitrum AB Antifibrinolytically active compounds

Also Published As

Publication number Publication date
AU5845294A (en) 1994-08-15
WO1994015904A1 (en) 1994-07-21
SE9300013D0 (en) 1992-12-30

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