JO2677B1 - Improved Process For The Preparation Of Clevudine As Anti-HBV Agent - Google Patents
Improved Process For The Preparation Of Clevudine As Anti-HBV AgentInfo
- Publication number
- JO2677B1 JO2677B1 JO2007521A JOP20070521A JO2677B1 JO 2677 B1 JO2677 B1 JO 2677B1 JO 2007521 A JO2007521 A JO 2007521A JO P20070521 A JOP20070521 A JO P20070521A JO 2677 B1 JO2677 B1 JO 2677B1
- Authority
- JO
- Jordan
- Prior art keywords
- clevudine
- preparation
- improved process
- arabinofuranosyl
- thymine
- Prior art date
Links
Classifications
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Gastroenterology & Hepatology (AREA)
- Epidemiology (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Saccharide Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Disclosed herein is an improved method for preparing 1-(2'-deoxy-2'-flouro- beta-L-arabinofuranosyl) thymine (clevudine)useful as an anti-HBV (hepatitis B virus)agent. The method comprises an improved purification process of 2-O-imidazolylsulfonyl-1.3.5-tri-O-benzoyl-alpha-L-ribofuranoside used as a key intermediate in the preparation of clevudine, and a final deprotection process using an alkaline metal salt, which is safe and easy to handle, as a deprotecting regent of 1-(3.5-di-O-benzoyl-2-deoxy-2-fluoro-beta-L-arabinofuranosyl)thymine so that productivity can be increased.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR1020060124497A KR100839322B1 (en) | 2006-12-08 | 2006-12-08 | Improved process for the preparation of clevudine as anti-hbv agent |
Publications (1)
Publication Number | Publication Date |
---|---|
JO2677B1 true JO2677B1 (en) | 2013-03-03 |
Family
ID=39492283
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JO2007521A JO2677B1 (en) | 2006-12-08 | 2007-12-06 | Improved Process For The Preparation Of Clevudine As Anti-HBV Agent |
Country Status (3)
Country | Link |
---|---|
KR (1) | KR100839322B1 (en) |
JO (1) | JO2677B1 (en) |
WO (1) | WO2008069451A1 (en) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN105943547B (en) * | 2016-05-23 | 2018-01-19 | 北京慧宝源生物技术股份有限公司 | The pharmaceutical composition of Anti-HBV activity and its application |
CN106831901A (en) * | 2016-12-14 | 2017-06-13 | 安徽省诚联医药科技有限公司 | The preparation method of the tri-benzoyl α D arabinofuranoses of 2 deoxidation, 2 fluorine 1,3,5 |
CN109467583A (en) * | 2018-11-17 | 2019-03-15 | 扬州工业职业技术学院 | A kind of green synthesis process of Clevudine |
-
2006
- 2006-12-08 KR KR1020060124497A patent/KR100839322B1/en active IP Right Grant
-
2007
- 2007-10-31 WO PCT/KR2007/005441 patent/WO2008069451A1/en active Application Filing
- 2007-12-06 JO JO2007521A patent/JO2677B1/en active
Also Published As
Publication number | Publication date |
---|---|
WO2008069451A1 (en) | 2008-06-12 |
KR100839322B1 (en) | 2008-06-17 |
KR20080052827A (en) | 2008-06-12 |
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