AU2001285958A1 - Method for obtaining 4-(n-alkylamine)-5, 6-dihydro-4h-thieno-(2,3-b)-thiopyran-2-sulfamide-7, 7-dioxides and intermediate products - Google Patents

Method for obtaining 4-(n-alkylamine)-5, 6-dihydro-4h-thieno-(2,3-b)-thiopyran-2-sulfamide-7, 7-dioxides and intermediate products

Info

Publication number
AU2001285958A1
AU2001285958A1 AU2001285958A AU8595801A AU2001285958A1 AU 2001285958 A1 AU2001285958 A1 AU 2001285958A1 AU 2001285958 A AU2001285958 A AU 2001285958A AU 8595801 A AU8595801 A AU 8595801A AU 2001285958 A1 AU2001285958 A1 AU 2001285958A1
Authority
AU
Australia
Prior art keywords
thiopyran
dioxides
dihydro
obtaining
alkylamine
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.)
Abandoned
Application number
AU2001285958A
Inventor
Pablo Garcia Losada
Antonio Lorente Bonde-Larson
Jorge Martin Juarez
Luis Octavio Silva Guisasola
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.)
Raga Consultores SL
Original Assignee
Raga Consultores SL
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 Raga Consultores SL filed Critical Raga Consultores SL
Publication of AU2001285958A1 publication Critical patent/AU2001285958A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • 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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

The process for obtaining 4-(N-alkylamino)-5,6-dihydro-4H-thien-(2,3-b)-thiopyran-2-sulfonamide- 7,7-dioxides (I) wherein R1 is H or C1-5 alkyl, and R2 is C1-5 alkyl, starts from the corresponding 4-(N-alkylamino)-5,6-dihydro-4H-thien-(2,3-b)-thiopyran-7,7-dioxides, and comprises protecting the alkylamine group, introducing a sulfonamide group and eliminating protecting group. Some compounds of formula (I) are inhibitors of the carbonic anhydrase and can be used in the treatment of elevated intraocular pressure. <CHEM>
AU2001285958A 2000-09-04 2001-09-04 Method for obtaining 4-(n-alkylamine)-5, 6-dihydro-4h-thieno-(2,3-b)-thiopyran-2-sulfamide-7, 7-dioxides and intermediate products Abandoned AU2001285958A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
ESP200002171 2000-09-04
ES200002171A ES2177415B1 (en) 2000-09-04 2000-09-04 PROCEDURE FOR OBTAINING 4-ALQUILAMINO-5, 6-DIHIDRO-4H-TIENO- (2,3B) -TIOPIRAN-2-SULFONAMIDE-7-DIOXIDES, AND INTERMEDIATES.
PCT/ES2001/000335 WO2002020529A1 (en) 2000-09-04 2001-09-04 Method for obtaining 4-(n-alkylamine)-5, 6-dihydro-4h-thieno-(2,3-b)-thiopyran-2-sulfamide-7, 7-dioxides and intermediate products

Publications (1)

Publication Number Publication Date
AU2001285958A1 true AU2001285958A1 (en) 2002-03-22

Family

ID=8494840

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2001285958A Abandoned AU2001285958A1 (en) 2000-09-04 2001-09-04 Method for obtaining 4-(n-alkylamine)-5, 6-dihydro-4h-thieno-(2,3-b)-thiopyran-2-sulfamide-7, 7-dioxides and intermediate products

Country Status (9)

Country Link
US (1) US7030250B2 (en)
EP (1) EP1329453B1 (en)
JP (1) JP5137284B2 (en)
AT (1) ATE269338T1 (en)
AU (1) AU2001285958A1 (en)
CA (1) CA2436185C (en)
DE (1) DE60103921T2 (en)
ES (2) ES2177415B1 (en)
WO (1) WO2002020529A1 (en)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1765828B1 (en) * 2004-07-09 2007-12-05 FDC Limited AN IMPROVED PROCESS FOR THE PREPARATION OF 5,6 -DIHYDRO -4H-4(S)-ETHYLAMINO-6(S)-METHYLTHIENO[2,3-b] THIOPYRAN-2-SULFONAMIDE- 7,7 -DIOXIDE AND ITS SALT
ES2253112B1 (en) * 2004-11-05 2007-03-16 Ragactives, S.L. PROCEDURE FOR OBTAINING DERIVATIVES OF 4- (N-ALQUILAMINO) -5, 6-DIHIDRO-4H-TIENO- (2,3-B) -TIOPIRANE.
US7109353B2 (en) * 2004-12-28 2006-09-19 Council Of Scientific And Industrial Research Process for preparing 5,6-dihydro-4-(S)-(ethylamino)-6-(S) methyl-4H-thieno[2,3b]thiopyran-2-sulphonamide-7,7-dioxide HCl
US20060155132A1 (en) * 2005-01-06 2006-07-13 Kovacs Laszlo Z Method of making dorzolamide hydrochloride
US20060173068A1 (en) * 2005-01-18 2006-08-03 Judith Aronhime Amorphous and crystalline forms of dorzolamide hydrochloride and processes of making same
CN1939923B (en) * 2005-09-30 2010-05-05 北京德众万全医药科技有限公司 Production of dozoan intermediate
LT5504B (en) 2006-08-02 2008-06-25 Biotechnologijos Institutas Benzimidazo[1,2-c][1,2,3]thiadiazol-7-sulfonamides as inhibitors of carbonic anhydrase and the intermediates for production thereof
WO2010013240A1 (en) 2008-07-31 2010-02-04 Dekel Pharmaceuticals Ltd. Compositions and methods for treating inflammatory disorders
KR20180058758A (en) 2015-09-22 2018-06-01 그레이버그 비젼, 인크. Compounds and compositions for the treatment of ocular disorders
CN110662543A (en) 2017-03-23 2020-01-07 灰色视觉公司 Medicaments and compositions for treating ocular diseases
MX2019013363A (en) 2017-05-10 2020-01-13 Graybug Vision Inc Extended release microparticles and suspensions thereof for medical therapy.
WO2020069353A1 (en) * 2018-09-27 2020-04-02 Graybug Vision, Inc. Compounds and compositions for ocular delivery
EP3908268A1 (en) * 2019-01-09 2021-11-17 Yeda Research and Development Co. Ltd Modulators of pin1 activity and uses thereof
CN113336770B (en) * 2021-06-24 2022-05-20 中南林业科技大学 Chiral synthesis method of dorzolamide hydrochloride

Family Cites Families (16)

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US4797413A (en) * 1986-05-14 1989-01-10 Merck & Co., Inc. Thieno thiopyran sulfonamide derivatives, pharmaceutical compositions and use
US4863922A (en) * 1984-12-12 1989-09-05 Merck & Co., Inc. Substituted aromatic sulfonamides as antiglaucoma agents, compositions and use
US4820848A (en) * 1984-12-12 1989-04-11 Merck & Co., Inc. Substituted aromatic sulfonamides as antiglaucoma agents
US4677115A (en) * 1984-12-12 1987-06-30 Merck & Co., Inc. Antiglaucoma thieno-thiopyran and thieno-thiepin sulfonamide derivatives, compositions, and method of use thereof
US4824968A (en) * 1984-12-12 1989-04-25 Merck & Co., Inc. Substituted aromatic sulfonamides as antiglaucoma agents
US5120757A (en) * 1989-07-31 1992-06-09 Merck & Co., Inc. Substituted aromatic sulfonamides as antiglaucoma agents
US5011942A (en) * 1990-02-05 1991-04-30 Merck & Co., Inc. Process for racemizing an enantiomer of 5,6-dihydro-4-alkylamino-4H-thieno(or furo) [2,3-B]-thiopyran-2-sulfonamide-7,7-dioxide
IE911192A1 (en) * 1990-04-12 1991-10-23 Merck & Co Inc Substituted aromatic sulfonamides as antiglaucoma agents
US5091409A (en) * 1990-05-17 1992-02-25 Merck & Co., Inc. 4-alkylamino-6-(C3-5 -hydrocarbyl)thieno[2,3-B]thiopyran-2-sulfonamide-7,7-dioxides
KR100319837B1 (en) 1992-08-28 2002-04-22 커스티 마가렛 핀더 Enzymatic Asymmetric Reduction Method for the Preparation of 4H-Tieno (2,3-6) thiopyran Derivatives
JP3279671B2 (en) 1992-09-28 2002-04-30 鐘淵化学工業株式会社 Method for producing thienothiopyran derivative
TW265343B (en) * 1993-03-22 1995-12-11 Merck & Co Inc
US5391772A (en) * 1993-07-08 1995-02-21 Merck & Co., Inc. Converting an alcohol to an azide with SN 2 inversion using a phosphoryl azide
US5441722A (en) * 1994-02-18 1995-08-15 Merck & Co., Inc. Short synthesis of 5,6-dihydro-(S)-4-(ethylamino)-(S)-6-[C3 H3 ]-4[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide and related non radioactive compounds
US5474919A (en) * 1994-09-13 1995-12-12 Merck & Co., Inc. Bioconversion process for the synthesis of transhydroxy sulfone by Rhodotorula rubra or Rhodotorula piliminae
US5760249A (en) * 1995-08-29 1998-06-02 Merck & Co., Inc. Synthesis of hydroxysulfone and related compounds

Also Published As

Publication number Publication date
US20030220509A1 (en) 2003-11-27
DE60103921D1 (en) 2004-07-22
CA2436185C (en) 2009-06-02
WO2002020529A1 (en) 2002-03-14
US7030250B2 (en) 2006-04-18
WO2002020529A8 (en) 2002-07-25
ES2223907T3 (en) 2005-03-01
JP2004508375A (en) 2004-03-18
ATE269338T1 (en) 2004-07-15
EP1329453B1 (en) 2004-06-16
EP1329453A1 (en) 2003-07-23
DE60103921T2 (en) 2005-06-30
JP5137284B2 (en) 2013-02-06
CA2436185A1 (en) 2002-03-14
ES2177415B1 (en) 2004-10-16
ES2177415A1 (en) 2002-12-01

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