ES2177415A1 - Procedimiento para la obtencion de 4-alquilamino-5, 6-dihidro-4h-tieno-(2,3b)-tiopiran-2-sulfonamida-7-dioxidos, e intermedios. - Google Patents
Procedimiento para la obtencion de 4-alquilamino-5, 6-dihidro-4h-tieno-(2,3b)-tiopiran-2-sulfonamida-7-dioxidos, e intermedios.Info
- Publication number
- ES2177415A1 ES2177415A1 ES200002171A ES200002171A ES2177415A1 ES 2177415 A1 ES2177415 A1 ES 2177415A1 ES 200002171 A ES200002171 A ES 200002171A ES 200002171 A ES200002171 A ES 200002171A ES 2177415 A1 ES2177415 A1 ES 2177415A1
- Authority
- ES
- Spain
- Prior art keywords
- thiopyran
- dioxides
- dihydro
- sulfonamide
- obtaining
- 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.)
- Granted
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
Procedimiento para la obtención de 4-alquilamino-5,6-dihidro-4H- tieno-(2,3b)-tiopiran-2-sulfonamida-7-dióxidos, e intermedios. El procedimiento para la obtención de 4-alquilamino-5,6-dihidro-4H- tieno-(2,3b)-tiopiran-2-sulfonamida-7,7-dióxidos (I) donde R1 es H o alquilo C1-5 y R2 es alquilo C1-5, parte de los correspondientes 4-alquilamino-5,6-dihidro-4H-tieno-(2,3b)- tiopiran-7,7-dióxidos y comprende la protección del grupo alquilamino, la introducción del grupo sulfonamida y la liberación del grupo protector. Algunos compuestos (I) son inhibidores de la anhidrasa carbónica y pueden ser utilizados en el tratamiento de la presión intraocular elevada.
Priority Applications (10)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
ES200002171A ES2177415B1 (es) | 2000-09-04 | 2000-09-04 | Procedimiento para la obtencion de 4-alquilamino-5, 6-dihidro-4h-tieno-(2,3b)-tiopiran-2-sulfonamida-7-dioxidos, e intermedios. |
AT01965290T ATE269338T1 (de) | 2000-09-04 | 2001-09-04 | Verfahren zur herstellung von 4-(n-alkylamin)-5,6-dihydro-4h-thieno-(2,3-b)-t iopyran-2-sulfonamid- 7,7-dioxiden und zwischenprodukte |
AU2001285958A 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 |
DE60103921T DE60103921T2 (de) | 2000-09-04 | 2001-09-04 | Verfahren zur herstellung von 4-(n-alkylamin)-5,6-dihydro-4h-thieno-(2,3-b)-thiopyran-2-sulfonamid-7,7-dioxiden und zwischenprodukte |
PCT/ES2001/000335 WO2002020529A1 (es) | 2000-09-04 | 2001-09-04 | PROCEDIMIENTO PARA LA OBTENCIÓN DE 4-(N-ALQUILAMINO)-5,6-DIHIDRO-4H-TIENO-(2,3-b)-TIOPIRAN-2-SULFONAMIDA-7,7-DIÓXIDOS, E INTERMEDIOS |
CA002436185A CA2436185C (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 |
JP2002525150A JP5137284B2 (ja) | 2000-09-04 | 2001-09-04 | 4−(N−アルキルアミノ)−5,6−ジヒドロ−4H−チエン−(2,3−b)−チオピラン−2−スルホンアミド−7,7−ジオキシドおよび中間体を得る方法 |
ES01965290T ES2223907T3 (es) | 2000-09-04 | 2001-09-04 | Procedimiento para la obtencion de 4-(n-alquilamino) -5,6-dihidro-4h-tieno-(2,3,b)-tiopiran-2-sulfonamida-7,7-dioxidos, e intermedios. |
EP01965290A EP1329453B1 (en) | 2000-09-04 | 2001-09-04 | Method for obtaining 4-(n-alkylamine)-5, 6-dihydro-4h-thieno-(2,3-b)-thiopyran-2-sulfonamide-7, 7-dioxides and intermediate products |
US10/379,096 US7030250B2 (en) | 2000-09-04 | 2003-03-03 | Process for obtaining 4-(N-alkylamino)-5,6-dihydro-4H-thien-(2,3-b)-thiopyran-2-sulfonamide-7,7-dioxides and intermediates |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
ES200002171A ES2177415B1 (es) | 2000-09-04 | 2000-09-04 | Procedimiento para la obtencion de 4-alquilamino-5, 6-dihidro-4h-tieno-(2,3b)-tiopiran-2-sulfonamida-7-dioxidos, e intermedios. |
Publications (2)
Publication Number | Publication Date |
---|---|
ES2177415A1 true ES2177415A1 (es) | 2002-12-01 |
ES2177415B1 ES2177415B1 (es) | 2004-10-16 |
Family
ID=8494840
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES200002171A Expired - Fee Related ES2177415B1 (es) | 2000-09-04 | 2000-09-04 | Procedimiento para la obtencion de 4-alquilamino-5, 6-dihidro-4h-tieno-(2,3b)-tiopiran-2-sulfonamida-7-dioxidos, e intermedios. |
ES01965290T Expired - Lifetime ES2223907T3 (es) | 2000-09-04 | 2001-09-04 | Procedimiento para la obtencion de 4-(n-alquilamino) -5,6-dihidro-4h-tieno-(2,3,b)-tiopiran-2-sulfonamida-7,7-dioxidos, e intermedios. |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES01965290T Expired - Lifetime ES2223907T3 (es) | 2000-09-04 | 2001-09-04 | Procedimiento para la obtencion de 4-(n-alquilamino) -5,6-dihidro-4h-tieno-(2,3,b)-tiopiran-2-sulfonamida-7,7-dioxidos, e intermedios. |
Country Status (9)
Country | Link |
---|---|
US (1) | US7030250B2 (es) |
EP (1) | EP1329453B1 (es) |
JP (1) | JP5137284B2 (es) |
AT (1) | ATE269338T1 (es) |
AU (1) | AU2001285958A1 (es) |
CA (1) | CA2436185C (es) |
DE (1) | DE60103921T2 (es) |
ES (2) | ES2177415B1 (es) |
WO (1) | WO2002020529A1 (es) |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2253112A1 (es) * | 2004-11-05 | 2006-05-16 | Ragactives, S.L. | Procedimiento para la obtencion de derivados de 4-(n-alquilamino)-5, 6-dihidro-4h-tieno-(2,3-b)-tiopirano. |
CN113336770A (zh) * | 2021-06-24 | 2021-09-03 | 中南林业科技大学 | 一种盐酸多佐胺的手性合成方法 |
Families Citing this family (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU2005290855B2 (en) * | 2004-07-09 | 2010-08-19 | Fdc Ltd | 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 |
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 |
WO2006074230A2 (en) * | 2005-01-06 | 2006-07-13 | Teva Gyógyszergyár Zártkörüen Müködö Részvénytársaság | Method of making dorzolamide hydrochloride |
JP2008526780A (ja) * | 2005-01-18 | 2008-07-24 | テバ ジョジセルジャール ザ−トケルエン ムケド レ−スベニュタ−ルシャシャ−グ | ドルゾルアミド塩酸塩の非晶質および結晶質の形態およびそれらを製造する方法 |
CN1939923B (zh) * | 2005-09-30 | 2010-05-05 | 北京德众万全医药科技有限公司 | 一种多佐胺中间体的制备方法 |
LT5504B (lt) | 2006-08-02 | 2008-06-25 | Biotechnologijos Institutas | Benzimidazo[1,2-c][1,2,3]tiadiazolo sulfonamidai - karboanhidrazių slopikliai ir tarpiniai junginiai jiems gauti |
EP2309858A4 (en) | 2008-07-31 | 2011-09-14 | Dekel Pharmaceuticals Ltd | COMPOSITIONS AND METHOD FOR THE TREATMENT OF INFLAMMATORY DISEASES |
JP2018536017A (ja) | 2015-09-22 | 2018-12-06 | グレイバグ ビジョン インコーポレイテッド | 眼障害の治療のための化合物及び組成物 |
AU2018240462C1 (en) | 2017-03-23 | 2022-12-08 | Graybug Vision, Inc. | Drugs and compositions for the treatment of ocular disorders |
US11160870B2 (en) | 2017-05-10 | 2021-11-02 | 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 |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0411704A1 (en) * | 1989-07-31 | 1991-02-06 | Merck & Co. Inc. | Substituted aromatic sulfonamides as antiglaucoma agents |
EP0452151A1 (en) * | 1990-04-12 | 1991-10-16 | Merck & Co. Inc. | Substituted aromatic sulfonamides as antiglaucoma agents |
EP0457586A1 (en) * | 1990-05-17 | 1991-11-21 | Merck & Co. Inc. | 4-alkylamino-6-(C3-5-hydrocarbyl)thieno [2,3-B] thiopyran-2-sulfonamide-7,7-dioxides |
EP0617037A1 (en) * | 1993-03-22 | 1994-09-28 | Merck & Co. Inc. | Enantioselective synthesis of thieno(2,3-b) thiopyran-7, 7-dioxide compounds |
Family Cites Families (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4863922A (en) * | 1984-12-12 | 1989-09-05 | Merck & Co., Inc. | Substituted aromatic sulfonamides as antiglaucoma agents, compositions and use |
US4797413A (en) * | 1986-05-14 | 1989-01-10 | Merck & Co., Inc. | Thieno thiopyran sulfonamide derivatives, pharmaceutical compositions and use |
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 |
US4820848A (en) * | 1984-12-12 | 1989-04-11 | Merck & Co., Inc. | Substituted aromatic sulfonamides as antiglaucoma agents |
US4824968A (en) * | 1984-12-12 | 1989-04-25 | 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 |
US5580764A (en) | 1992-08-28 | 1996-12-03 | Zeneca Limited | Process for microbial reduction producing 4(S)-hydroxy-6(S)methyl-thienopyran derivatives |
JP3279671B2 (ja) | 1992-09-28 | 2002-04-30 | 鐘淵化学工業株式会社 | チエノチオピラン誘導体の製造方法 |
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 |
-
2000
- 2000-09-04 ES ES200002171A patent/ES2177415B1/es not_active Expired - Fee Related
-
2001
- 2001-09-04 CA CA002436185A patent/CA2436185C/en not_active Expired - Fee Related
- 2001-09-04 JP JP2002525150A patent/JP5137284B2/ja not_active Expired - Fee Related
- 2001-09-04 WO PCT/ES2001/000335 patent/WO2002020529A1/es active IP Right Grant
- 2001-09-04 AU AU2001285958A patent/AU2001285958A1/en not_active Abandoned
- 2001-09-04 AT AT01965290T patent/ATE269338T1/de not_active IP Right Cessation
- 2001-09-04 DE DE60103921T patent/DE60103921T2/de not_active Expired - Lifetime
- 2001-09-04 EP EP01965290A patent/EP1329453B1/en not_active Expired - Lifetime
- 2001-09-04 ES ES01965290T patent/ES2223907T3/es not_active Expired - Lifetime
-
2003
- 2003-03-03 US US10/379,096 patent/US7030250B2/en not_active Expired - Fee Related
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0411704A1 (en) * | 1989-07-31 | 1991-02-06 | Merck & Co. Inc. | Substituted aromatic sulfonamides as antiglaucoma agents |
EP0452151A1 (en) * | 1990-04-12 | 1991-10-16 | Merck & Co. Inc. | Substituted aromatic sulfonamides as antiglaucoma agents |
EP0457586A1 (en) * | 1990-05-17 | 1991-11-21 | Merck & Co. Inc. | 4-alkylamino-6-(C3-5-hydrocarbyl)thieno [2,3-B] thiopyran-2-sulfonamide-7,7-dioxides |
EP0617037A1 (en) * | 1993-03-22 | 1994-09-28 | Merck & Co. Inc. | Enantioselective synthesis of thieno(2,3-b) thiopyran-7, 7-dioxide compounds |
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2253112A1 (es) * | 2004-11-05 | 2006-05-16 | Ragactives, S.L. | Procedimiento para la obtencion de derivados de 4-(n-alquilamino)-5, 6-dihidro-4h-tieno-(2,3-b)-tiopirano. |
WO2006051137A1 (es) * | 2004-11-05 | 2006-05-18 | Ragactives, S.L. | PROCEDIMIENTO PARA LA OBTENCIÓN DE DERIVADOS DE 4-(N-ALQUILAMINO)-5,6-DIHIDRO-4H-TIENO-[2,3-b]-TIOPIRANO |
CN113336770A (zh) * | 2021-06-24 | 2021-09-03 | 中南林业科技大学 | 一种盐酸多佐胺的手性合成方法 |
CN113336770B (zh) * | 2021-06-24 | 2022-05-20 | 中南林业科技大学 | 一种盐酸多佐胺的手性合成方法 |
Also Published As
Publication number | Publication date |
---|---|
ES2177415B1 (es) | 2004-10-16 |
JP5137284B2 (ja) | 2013-02-06 |
JP2004508375A (ja) | 2004-03-18 |
US20030220509A1 (en) | 2003-11-27 |
US7030250B2 (en) | 2006-04-18 |
EP1329453A1 (en) | 2003-07-23 |
DE60103921T2 (de) | 2005-06-30 |
AU2001285958A1 (en) | 2002-03-22 |
ES2223907T3 (es) | 2005-03-01 |
ATE269338T1 (de) | 2004-07-15 |
EP1329453B1 (en) | 2004-06-16 |
WO2002020529A8 (es) | 2002-07-25 |
CA2436185C (en) | 2009-06-02 |
WO2002020529A1 (es) | 2002-03-14 |
DE60103921D1 (de) | 2004-07-22 |
CA2436185A1 (en) | 2002-03-14 |
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