ATE316963T1 - Herstellung von sulfonamiden - Google Patents
Herstellung von sulfonamidenInfo
- Publication number
- ATE316963T1 ATE316963T1 AT00903628T AT00903628T ATE316963T1 AT E316963 T1 ATE316963 T1 AT E316963T1 AT 00903628 T AT00903628 T AT 00903628T AT 00903628 T AT00903628 T AT 00903628T AT E316963 T1 ATE316963 T1 AT E316963T1
- Authority
- AT
- Austria
- Prior art keywords
- lower alkyl
- hydrogen
- hydroxy
- alkoxy
- alkyl
- Prior art date
Links
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 13
- -1 methylenedioxy, ethylenedioxy Chemical group 0.000 abstract 9
- 125000003545 alkoxy group Chemical group 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 7
- 239000001257 hydrogen Substances 0.000 abstract 7
- 150000002431 hydrogen Chemical group 0.000 abstract 6
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 5
- 125000004414 alkyl thio group Chemical group 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical class 0.000 abstract 4
- 229910052784 alkaline earth metal Inorganic materials 0.000 abstract 2
- 150000001342 alkaline earth metals Chemical class 0.000 abstract 2
- 125000003282 alkyl amino group Chemical group 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 229910052751 metal Inorganic materials 0.000 abstract 2
- 239000002184 metal Substances 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 125000006239 protecting group Chemical group 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 abstract 1
- 125000005194 alkoxycarbonyloxy group Chemical group 0.000 abstract 1
- 125000004644 alkyl sulfinyl group Chemical group 0.000 abstract 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 1
- 150000001450 anions Chemical class 0.000 abstract 1
- 125000001769 aryl amino group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000005110 aryl thio group Chemical group 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 abstract 1
- 150000004820 halides Chemical class 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000006216 methylsulfinyl group Chemical group [H]C([H])([H])S(*)=O 0.000 abstract 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 229940124530 sulfonamide Drugs 0.000 abstract 1
- 150000003456 sulfonamides Chemical class 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/52—Two oxygen atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/69—Benzenesulfonamido-pyrimidines
-
- 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)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Epidemiology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP00903628A EP1254121B1 (de) | 2000-01-25 | 2000-01-25 | Herstellung von sulfonamiden |
| PCT/EP2000/000556 WO2001055120A1 (en) | 2000-01-25 | 2000-01-25 | Preparation of sulfonamides |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE316963T1 true ATE316963T1 (de) | 2006-02-15 |
Family
ID=8163805
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT00903628T ATE316963T1 (de) | 2000-01-25 | 2000-01-25 | Herstellung von sulfonamiden |
Country Status (13)
| Country | Link |
|---|---|
| EP (1) | EP1254121B1 (de) |
| JP (1) | JP3751882B2 (de) |
| KR (1) | KR100495550B1 (de) |
| CN (1) | CN1178921C (de) |
| AT (1) | ATE316963T1 (de) |
| AU (1) | AU2000225442A1 (de) |
| CA (1) | CA2397258C (de) |
| DE (1) | DE60025803T2 (de) |
| DK (1) | DK1254121T3 (de) |
| ES (1) | ES2255973T3 (de) |
| MX (1) | MXPA02007192A (de) |
| PT (1) | PT1254121E (de) |
| WO (1) | WO2001055120A1 (de) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2686457A1 (en) * | 2007-05-08 | 2008-11-13 | Generics [Uk] Limited | Novel polymorphic forms |
| US8664390B2 (en) | 2007-06-29 | 2014-03-04 | Generics (Uk) Limited | Process for the introduction of hydroxyethoxy side chain in bosentan |
| NZ585438A (en) * | 2007-10-24 | 2012-09-28 | Generics Uk Ltd | Novel crystalline forms of 4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(2-pyrimidinyl)-pyrimidin-4-yI]-benzenesulfonamide |
| EP2248805A3 (de) * | 2008-01-01 | 2011-02-23 | Cipla Ltd. | Verfahren zur Herstellung von Bosentan, dessen polymorphe Formen und Salze |
| EP2240469A2 (de) | 2008-01-24 | 2010-10-20 | Actavis Group PTC EHF | Substantiell reine und stabile kristalline form von bosentan |
| CA2712860C (en) | 2008-02-08 | 2014-11-18 | Abhay Gaitonde | Process for preparing bosentan |
| CN101279948B (zh) * | 2008-03-14 | 2010-08-11 | 苏州博鸿化工技术有限公司 | 4,6-二氯-5-(2-甲氧基苯氧基)-2,2'-二嘧啶的合成方法 |
| WO2010015623A1 (en) * | 2008-08-05 | 2010-02-11 | Farmaprojects, S. A. | Process for the preparation of endothelin receptor antagonists |
| US20110263623A1 (en) | 2008-08-12 | 2011-10-27 | Cadila Healthcare Limited | Process for preparation of bosentan |
| CA2741928A1 (en) | 2008-11-03 | 2010-06-03 | Generics [Uk] Limited | Hplc method for the analysis of bosentan and related substances and use of these substances as reference standards and markers |
| IT1393136B1 (it) * | 2009-03-11 | 2012-04-11 | Sifa Vitor S R L | Procedimento per la preparazione del bosentan |
| RU2011145813A (ru) * | 2009-04-13 | 2013-05-20 | Сандох Аг | Способ получения антагониста эндотелиального рецептора (бозентана) |
| EP2368884A1 (de) | 2010-03-25 | 2011-09-28 | Laboratorios Lesvi, S.L. | Verfahren zur Herstellung von Bosentan |
| JP6129739B2 (ja) | 2010-10-01 | 2017-05-17 | ザック システム エス.ピー.エー.ZaCh System S.p.A. | ボセンタン一水和物及びその中間体の製造方法 |
| JP2015503555A (ja) * | 2012-05-11 | 2015-02-02 | ハナル・バイオファーマ・カンパニー・リミテッド | ボセンタン制御放出性経口製剤 |
| KR102004422B1 (ko) * | 2012-12-20 | 2019-07-26 | 제일약품주식회사 | 보센탄 일수화물의 제조방법, 이에 사용되는 신규 중간체 및 이의 제조방법 |
| AR095727A1 (es) * | 2013-03-27 | 2015-11-04 | Actelion Pharmaceuticals Ltd | Preparación de intermediarios de pirimidina |
| CN114907275A (zh) * | 2022-04-29 | 2022-08-16 | 武汉工程大学 | 一种波生坦的制备方法 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2086544C1 (ru) * | 1991-06-13 | 1997-08-10 | Хоффманн-Ля Рош АГ | Бензолсульфонамидные производные пиримидина или их соли, фармацевтическая композиция для лечения заболеваний, связанных с активностью эндотелина |
| TW287160B (de) * | 1992-12-10 | 1996-10-01 | Hoffmann La Roche | |
| HUT77534A (hu) * | 1994-12-28 | 1998-05-28 | Kowa Co. Ltd. | Pirimidinszármazékok és ezeket tartalmazó gyógyszerkészítmények |
| US5739333A (en) * | 1995-05-16 | 1998-04-14 | Tanabe Seiyaku Co., Ltd. | Sulfonamide derivative and process for preparing the same |
| KR100453097B1 (ko) * | 1995-09-06 | 2004-12-31 | 코와 가부시키가이샤 | 피리미딘유도체 |
-
2000
- 2000-01-25 MX MXPA02007192A patent/MXPA02007192A/es active IP Right Grant
- 2000-01-25 KR KR10-2002-7009505A patent/KR100495550B1/ko not_active Expired - Lifetime
- 2000-01-25 DK DK00903628T patent/DK1254121T3/da active
- 2000-01-25 ES ES00903628T patent/ES2255973T3/es not_active Expired - Lifetime
- 2000-01-25 AT AT00903628T patent/ATE316963T1/de active
- 2000-01-25 WO PCT/EP2000/000556 patent/WO2001055120A1/en not_active Ceased
- 2000-01-25 EP EP00903628A patent/EP1254121B1/de not_active Expired - Lifetime
- 2000-01-25 CA CA002397258A patent/CA2397258C/en not_active Expired - Lifetime
- 2000-01-25 CN CNB00818643XA patent/CN1178921C/zh not_active Expired - Lifetime
- 2000-01-25 JP JP2001555062A patent/JP3751882B2/ja not_active Expired - Lifetime
- 2000-01-25 DE DE60025803T patent/DE60025803T2/de not_active Expired - Lifetime
- 2000-01-25 PT PT00903628T patent/PT1254121E/pt unknown
- 2000-01-25 AU AU2000225442A patent/AU2000225442A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| DK1254121T3 (da) | 2006-06-12 |
| EP1254121B1 (de) | 2006-02-01 |
| ES2255973T3 (es) | 2006-07-16 |
| DE60025803T2 (de) | 2006-11-02 |
| CA2397258C (en) | 2007-07-03 |
| EP1254121A1 (de) | 2002-11-06 |
| WO2001055120A1 (en) | 2001-08-02 |
| KR100495550B1 (ko) | 2005-06-16 |
| JP3751882B2 (ja) | 2006-03-01 |
| AU2000225442A1 (en) | 2001-08-07 |
| PT1254121E (pt) | 2006-06-30 |
| CN1425007A (zh) | 2003-06-18 |
| JP2003520857A (ja) | 2003-07-08 |
| CA2397258A1 (en) | 2001-08-02 |
| KR20020070511A (ko) | 2002-09-09 |
| DE60025803D1 (de) | 2006-04-13 |
| MXPA02007192A (es) | 2002-12-09 |
| CN1178921C (zh) | 2004-12-08 |
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