ATE162530T1 - 5-methyluridin-verfahren zur herstellung von 2',3'-didehydro-3'-desoxythymidin (d4t) im grossmassstab - Google Patents
5-methyluridin-verfahren zur herstellung von 2',3'-didehydro-3'-desoxythymidin (d4t) im grossmassstabInfo
- Publication number
- ATE162530T1 ATE162530T1 AT94402484T AT94402484T ATE162530T1 AT E162530 T1 ATE162530 T1 AT E162530T1 AT 94402484 T AT94402484 T AT 94402484T AT 94402484 T AT94402484 T AT 94402484T AT E162530 T1 ATE162530 T1 AT E162530T1
- Authority
- AT
- Austria
- Prior art keywords
- methyluridine
- didehydro
- desoxythymidine
- producing
- large scale
- Prior art date
Links
- XNKLLVCARDGLGL-JGVFFNPUSA-N Stavudine Chemical compound O=C1NC(=O)C(C)=CN1[C@H]1C=C[C@@H](CO)O1 XNKLLVCARDGLGL-JGVFFNPUSA-N 0.000 title abstract 5
- 238000000034 method Methods 0.000 title abstract 3
- DWRXFEITVBNRMK-UHFFFAOYSA-N Beta-D-1-Arabinofuranosylthymine Natural products O=C1NC(=O)C(C)=CN1C1C(O)C(O)C(CO)O1 DWRXFEITVBNRMK-UHFFFAOYSA-N 0.000 title abstract 2
- DWRXFEITVBNRMK-JXOAFFINSA-N ribothymidine Chemical compound O=C1NC(=O)C(C)=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](CO)O1 DWRXFEITVBNRMK-JXOAFFINSA-N 0.000 title abstract 2
- 238000010511 deprotection reaction Methods 0.000 abstract 1
- 238000002955 isolation Methods 0.000 abstract 1
- 238000011031 large-scale manufacturing process Methods 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 238000000746 purification Methods 0.000 abstract 1
Classifications
- 
        - C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
 
- 
        - A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
 
- 
        - A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
 
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Virology (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Communicable Diseases (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Animal Behavior & Ethology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title | 
|---|---|---|---|
| US15277893A | 1993-11-15 | 1993-11-15 | |
| US15305893A | 1993-11-15 | 1993-11-15 | |
| US08/309,637 US5672698A (en) | 1993-11-15 | 1994-09-23 | Preparation of 2',3'-didehydro-3'-deoxythymidine from 5-methyluridine | 
Publications (1)
| Publication Number | Publication Date | 
|---|---|
| ATE162530T1 true ATE162530T1 (de) | 1998-02-15 | 
Family
ID=27387314
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date | 
|---|---|---|---|
| AT94402484T ATE162530T1 (de) | 1993-11-15 | 1994-11-03 | 5-methyluridin-verfahren zur herstellung von 2',3'-didehydro-3'-desoxythymidin (d4t) im grossmassstab | 
Country Status (17)
| Country | Link | 
|---|---|
| US (1) | US5672698A (OSRAM) | 
| EP (1) | EP0653436B1 (OSRAM) | 
| JP (2) | JP3653292B2 (OSRAM) | 
| KR (1) | KR100329525B1 (OSRAM) | 
| CN (2) | CN1040115C (OSRAM) | 
| AT (1) | ATE162530T1 (OSRAM) | 
| AU (1) | AU686672B2 (OSRAM) | 
| CA (1) | CA2135852C (OSRAM) | 
| DE (1) | DE69408099T2 (OSRAM) | 
| DK (1) | DK0653436T3 (OSRAM) | 
| ES (1) | ES2113626T3 (OSRAM) | 
| FI (1) | FI115971B (OSRAM) | 
| GR (1) | GR3026638T3 (OSRAM) | 
| HU (2) | HU222118B1 (OSRAM) | 
| IL (1) | IL111569A (OSRAM) | 
| SG (1) | SG63554A1 (OSRAM) | 
| TW (1) | TW291480B (OSRAM) | 
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title | 
|---|---|---|---|---|
| US5608049A (en) * | 1995-03-10 | 1997-03-04 | Bristol-Myers Squibb Company | Preparation of d4T from 5-methyluridine | 
| US5608048A (en) * | 1995-06-05 | 1997-03-04 | Bristol-Myers Squibb Company | d4 T polymorphic Form 1 process | 
| US7034009B2 (en) * | 1995-10-26 | 2006-04-25 | Sirna Therapeutics, Inc. | Enzymatic nucleic acid-mediated treatment of ocular diseases or conditions related to levels of vascular endothelial growth factor receptor (VEGF-R) | 
| US6482805B2 (en) | 1998-03-25 | 2002-11-19 | Parker Hughes Institute | AZT derivatives exhibiting spermicidal and anti-viral activity | 
| US6191120B1 (en) | 1998-03-25 | 2001-02-20 | Wayne Hughes Institute | Spermicidally active 5-halo-6-alkoxy-5,6-dihydro-2′,3′-dideoxy-uridines and their pharamaceutical compositions | 
| US7144874B2 (en) * | 2002-10-25 | 2006-12-05 | Parker Hughes Institute | Aryl phosphate derivatives of d4T having activity against resistant HIV strains | 
| US20070015733A1 (en) * | 1998-06-29 | 2007-01-18 | Parker Hughes Institute | Aryl Phosphate Derivatives of d4T having Activity Against Resistant HIV Strains | 
| US6030957A (en) * | 1998-06-29 | 2000-02-29 | Wayne Hughes Institute | Aryl phosphate derivatives of d4T having anti-HIV activity | 
| CN1055293C (zh) * | 1998-10-06 | 2000-08-09 | 中国人民解放军第二军医大学 | 一种β-胸苷的制备方法 | 
| AU2001285197A1 (en) * | 2000-09-06 | 2002-03-22 | Bristol-Myers Squibb Company | Stavudine polymorphic form 1 process | 
| US6825177B2 (en) * | 2000-10-30 | 2004-11-30 | Parker Hughes Institute | Aryl phosphate derivatives of d4T with potent anti-viral activity | 
| PT1334108E (pt) * | 2000-11-13 | 2005-08-31 | Parker Hughes Inst | Derivados arilfosfato da d4t | 
| US20050131224A1 (en) * | 2003-12-15 | 2005-06-16 | Cti Pet Systems, Inc. | Method for preparing radiolabeled thymidine | 
| US7160537B2 (en) * | 2003-12-15 | 2007-01-09 | Siemens Medical Solutions Usa, Inc. | Method for preparing radiolabeled thymidine having low chromophoric byproducts | 
| US20060046972A1 (en) * | 2004-08-31 | 2006-03-02 | Parker Hughes Institute | Cytotoxic nucleoside analog compound 003 for treating cancer | 
| CN102180925B (zh) * | 2011-03-22 | 2013-05-08 | 苏州迪马生物科技发展有限公司 | 5-甲基尿苷合成工艺中乳化层的处理方法 | 
| CN104926902A (zh) * | 2014-03-17 | 2015-09-23 | 张容霞 | 2`-取代-2,2`-脱水尿苷或2`-取代-2,2`-脱水胞苷化合物及其制备方法和用途 | 
| CN106967767B (zh) * | 2017-04-25 | 2019-09-24 | 苏州笃美生物科技有限公司 | 一种β-胸苷的合成方法 | 
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title | 
|---|---|---|---|---|
| YU110888A (en) * | 1987-06-10 | 1989-08-31 | Wellcome Found | Process for obtaining timine derivatives | 
| US4921950A (en) * | 1988-06-09 | 1990-05-01 | Burroughs Wellcome Co. | Preparation of 3'azido-3-'-deoxythymidine | 
| JP3128080B2 (ja) * | 1991-10-02 | 2001-01-29 | 日本製紙株式会社 | 核酸化合物の新規な製造方法 | 
- 
        1994
        - 1994-09-23 US US08/309,637 patent/US5672698A/en not_active Expired - Lifetime
- 1994-10-26 TW TW083109889A patent/TW291480B/zh not_active IP Right Cessation
- 1994-11-03 EP EP94402484A patent/EP0653436B1/en not_active Expired - Lifetime
- 1994-11-03 SG SG1996002037A patent/SG63554A1/en unknown
- 1994-11-03 DK DK94402484T patent/DK0653436T3/da active
- 1994-11-03 DE DE69408099T patent/DE69408099T2/de not_active Expired - Lifetime
- 1994-11-03 AT AT94402484T patent/ATE162530T1/de active
- 1994-11-03 ES ES94402484T patent/ES2113626T3/es not_active Expired - Lifetime
- 1994-11-09 IL IL11156994A patent/IL111569A/en not_active IP Right Cessation
- 1994-11-11 FI FI945323A patent/FI115971B/fi not_active IP Right Cessation
- 1994-11-14 HU HU0105348A patent/HU222118B1/hu not_active IP Right Cessation
- 1994-11-14 AU AU78804/94A patent/AU686672B2/en not_active Ceased
- 1994-11-14 KR KR1019940029820A patent/KR100329525B1/ko not_active Expired - Fee Related
- 1994-11-14 HU HU9403257A patent/HU222119B1/hu not_active IP Right Cessation
- 1994-11-15 CN CN94119934A patent/CN1040115C/zh not_active Expired - Fee Related
- 1994-11-15 JP JP31543394A patent/JP3653292B2/ja not_active Expired - Fee Related
- 1994-11-15 CA CA002135852A patent/CA2135852C/en not_active Expired - Fee Related
 
- 
        1997
        - 1997-08-26 CN CN97117784A patent/CN1055477C/zh not_active Expired - Fee Related
 
- 
        1998
        - 1998-04-14 GR GR980400839T patent/GR3026638T3/el unknown
 
- 
        2004
        - 2004-12-24 JP JP2004373339A patent/JP2005139197A/ja active Pending
 
Also Published As
| Publication number | Publication date | 
|---|---|
| US5672698A (en) | 1997-09-30 | 
| CN1193021A (zh) | 1998-09-16 | 
| KR100329525B1 (ko) | 2002-11-14 | 
| CN1112123A (zh) | 1995-11-22 | 
| KR950014132A (ko) | 1995-06-15 | 
| TW291480B (OSRAM) | 1996-11-21 | 
| HUT69172A (en) | 1995-08-28 | 
| JP3653292B2 (ja) | 2005-05-25 | 
| SG63554A1 (en) | 1999-03-30 | 
| JPH07206856A (ja) | 1995-08-08 | 
| AU686672B2 (en) | 1998-02-12 | 
| FI945323A0 (fi) | 1994-11-11 | 
| GR3026638T3 (en) | 1998-07-31 | 
| HU222118B1 (hu) | 2003-04-28 | 
| HU0105348D0 (en) | 2002-02-28 | 
| DE69408099T2 (de) | 1998-09-03 | 
| JP2005139197A (ja) | 2005-06-02 | 
| CN1040115C (zh) | 1998-10-07 | 
| FI115971B (fi) | 2005-08-31 | 
| CA2135852C (en) | 2006-01-03 | 
| DK0653436T3 (da) | 1998-09-14 | 
| AU7880494A (en) | 1995-06-01 | 
| FI945323L (fi) | 1995-05-16 | 
| ES2113626T3 (es) | 1998-05-01 | 
| IL111569A (en) | 2001-03-19 | 
| CN1055477C (zh) | 2000-08-16 | 
| EP0653436A1 (en) | 1995-05-17 | 
| IL111569A0 (en) | 1995-01-24 | 
| HU222119B1 (hu) | 2003-04-28 | 
| CA2135852A1 (en) | 1995-05-16 | 
| EP0653436B1 (en) | 1998-01-21 | 
| HU9403257D0 (en) | 1995-01-30 | 
| DE69408099D1 (de) | 1998-02-26 | 
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Legal Events
| Date | Code | Title | Description | 
|---|---|---|---|
| UEP | Publication of translation of european patent specification |