ES2113845T3 - Procedimiento de preparacion de intermediarios utiles en la preparacion de 2',2'-difluoronucleosidos. - Google Patents
Procedimiento de preparacion de intermediarios utiles en la preparacion de 2',2'-difluoronucleosidos.Info
- Publication number
- ES2113845T3 ES2113845T3 ES88307750T ES88307750T ES2113845T3 ES 2113845 T3 ES2113845 T3 ES 2113845T3 ES 88307750 T ES88307750 T ES 88307750T ES 88307750 T ES88307750 T ES 88307750T ES 2113845 T3 ES2113845 T3 ES 2113845T3
- Authority
- ES
- Spain
- Prior art keywords
- difluoronucleosides
- preparation
- deoxy
- procedure
- erythro
- 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.)
- Expired - Lifetime
Links
- 238000000034 method Methods 0.000 title abstract 3
- 150000002596 lactones Chemical class 0.000 abstract 3
- ULGZDMOVFRHVEP-RWJQBGPGSA-N Erythromycin Chemical class O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 ULGZDMOVFRHVEP-RWJQBGPGSA-N 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 239000000543 intermediate Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 150000007522 mineralic acids Chemical class 0.000 abstract 1
- 150000007524 organic acids Chemical class 0.000 abstract 1
- 239000002243 precursor Substances 0.000 abstract 1
- 150000003839 salts Chemical class 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/26—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D307/30—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D307/32—Oxygen atoms
- C07D307/33—Oxygen atoms in position 2, the oxygen atom being in its keto or unsubstituted enol form
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- 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)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Saccharide Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Furan Compounds (AREA)
- Epoxy Compounds (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Polymers With Sulfur, Phosphorus Or Metals In The Main Chain (AREA)
Abstract
LA PRESENTE INVENCION DESCRIBE UN PROCESO PARA LA PREPARACION DE LACTAMAS INTERMEDIAS EN LA PRODUCCION DE 2,''2''DIFLUORONUCLEOSIDOS DE FORMA QUE QUEDE SUSTANCIALMENTE REDUCIDA REVERSION HACIA LA FORMA LACTONA DE CADENA ABIERTA, Y EL ENANTIOMERO ERITRO DESEADO PUEDE SER AISLADO SELECTIVAMENTE A PARTIR DE UNA MEZCLA ENANTIOMERICA DE ERITRO Y TREOLACTONAS EN FORMA CRISTALINA. TAMBIEN SE DESCRIBE UN PROCESO PARA LA PRODUCCION DE 2''- DEOXI - 2'',2''- DIFLUORONUCLEOSIDOS EN UNA RELACION ANOMERICA ALFA/BETA APROXIMADA DE 1:1, ASI COMO PROCESOS PARA AISLAR SELECTIVAMENTE BETA - 2''- DEOXI 2''2''-DIFLUOROCITIDINA, UNA SAL DE ADICION DE UN ACIDO ORGANICO O INORGANICO DERIVADO DE ESTA, A PARTIR DE UNA MEZCLA ALFA/BETA 1:1.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US9072587A | 1987-08-28 | 1987-08-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2113845T3 true ES2113845T3 (es) | 1998-05-16 |
Family
ID=22224017
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES95201846T Expired - Lifetime ES2157289T3 (es) | 1987-08-28 | 1988-08-22 | Procedimiento para la preparacion de 2'-desoxi-2',2'-difluoronucleosidos. |
| ES88307750T Expired - Lifetime ES2113845T3 (es) | 1987-08-28 | 1988-08-22 | Procedimiento de preparacion de intermediarios utiles en la preparacion de 2',2'-difluoronucleosidos. |
| ES95201845T Expired - Lifetime ES2176279T3 (es) | 1987-08-28 | 1988-08-22 | Procedimiento estereoselectivo para preparar 2`-2`-difluorolactonen protegidos. |
| ES94202041T Expired - Lifetime ES2131152T3 (es) | 1987-08-28 | 1988-08-22 | Procedimiento para aislar selectivamente beta-2'-desoxi-2',2'-difluorocitidina o sus sales. |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES95201846T Expired - Lifetime ES2157289T3 (es) | 1987-08-28 | 1988-08-22 | Procedimiento para la preparacion de 2'-desoxi-2',2'-difluoronucleosidos. |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES95201845T Expired - Lifetime ES2176279T3 (es) | 1987-08-28 | 1988-08-22 | Procedimiento estereoselectivo para preparar 2`-2`-difluorolactonen protegidos. |
| ES94202041T Expired - Lifetime ES2131152T3 (es) | 1987-08-28 | 1988-08-22 | Procedimiento para aislar selectivamente beta-2'-desoxi-2',2'-difluorocitidina o sus sales. |
Country Status (11)
| Country | Link |
|---|---|
| EP (4) | EP0688782B1 (es) |
| JP (5) | JP2738540B2 (es) |
| KR (1) | KR970002659B1 (es) |
| AT (4) | ATE202113T1 (es) |
| CA (1) | CA1324128C (es) |
| DE (4) | DE3856158T2 (es) |
| ES (4) | ES2157289T3 (es) |
| GR (1) | GR3026611T3 (es) |
| HU (3) | HU202249B (es) |
| IE (1) | IE81131B1 (es) |
| IL (1) | IL87517A (es) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2012129A1 (en) * | 1989-03-20 | 1990-09-20 | Ramakrishnan Nagarajan | Recovery of difluoro sugar |
| US5256797A (en) * | 1992-06-22 | 1993-10-26 | Eli Lilly And Company | Process for separating 2-deoxy-2,2-difluoro-D-ribofuranosyl alkylsulfonate anomers |
| US5401861A (en) * | 1992-06-22 | 1995-03-28 | Eli Lilly And Company | Low temperature process for preparing alpha-anomer enriched 2-deoxy-2,2-difluoro-D-ribofuranosyl sulfonates |
| US5252756A (en) * | 1992-06-22 | 1993-10-12 | Eli Lilly And Company | Process for preparing beta-anomer enriched 2-deoxy-2,2-difluoro-D-ribofuranosyl-arylsulfonates |
| UA41261C2 (uk) * | 1992-06-22 | 2001-09-17 | Елі Ліллі Енд Компані | Спосіб одержання збагачених бета-аномером нуклеозидів |
| YU43193A (sh) * | 1992-06-22 | 1997-01-08 | Eli Lilly And Company | 2'-deoksi-2',2'-difluoro(4-supstituisani)pirimidinski nukleozidi antivirusnog i antikancerogenog dejstva i međuproizvodi |
| US5256798A (en) * | 1992-06-22 | 1993-10-26 | Eli Lilly And Company | Process for preparing alpha-anomer enriched 2-deoxy-2,2-difluoro-D-ribofuranosyl sulfonates |
| US5559222A (en) * | 1995-02-03 | 1996-09-24 | Eli Lilly And Company | Preparation of 1-(2'-deoxy-2',2'-difluoro-D-ribo-pentofuranosyl)-cytosine from 2-deoxy-2,2-difluoro-β-D-ribo-pentopyranose |
| JP2000501738A (ja) | 1995-12-13 | 2000-02-15 | イーライ・リリー・アンド・カンパニー | α,α―ジフルオロ―β―ヒドロキシチオールエステル及びその合成 |
| KR100578616B1 (ko) * | 2004-07-23 | 2006-05-10 | 한미약품 주식회사 | D-에리트로-2,2-다이플루오로-2-데옥시-1-옥소라이보스화합물의 제조방법 |
| EP1940859A1 (en) * | 2005-10-28 | 2008-07-09 | Arch Pharmalabs Limited | An improved process for preparation of gemcitabine hydrochloride |
| KR101259648B1 (ko) * | 2005-12-14 | 2013-05-09 | 동아에스티 주식회사 | 2′,2′-디플루오로뉴클레오시드 및 중간체의 새로운 제조방법 |
| KR100741310B1 (ko) * | 2006-08-01 | 2007-08-01 | (주) 유일팜테크 | 젬시타빈의 합성에 유용한 신규한나프탈렌-2-카르복실레이트 유도체와 그의 제조방법 |
| EP2139884B1 (en) * | 2007-03-23 | 2013-12-04 | Dongwoo Syntech Co., Ltd. | Process for preparing of 2'-deoxy-2'2'-difluorocytidine |
| JP2011524369A (ja) | 2008-06-12 | 2011-09-01 | サイノファーム タイワン リミテッド | ゲムシタビン塩基の結晶多形 |
| GB0812895D0 (en) | 2008-07-15 | 2008-08-20 | Glycom As | Crystalline carbohydrate derivative |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4526988A (en) | 1983-03-10 | 1985-07-02 | Eli Lilly And Company | Difluoro antivirals and intermediate therefor |
| EP0184365B1 (en) * | 1984-12-04 | 1993-08-04 | Eli Lilly And Company | Improvements in the treatment of tumors in mammals |
| CA1295998C (en) * | 1985-07-29 | 1992-02-18 | Sai P. Sunkara | Nucleosides and their use as antineoplastic agents |
-
1988
- 1988-08-22 ES ES95201846T patent/ES2157289T3/es not_active Expired - Lifetime
- 1988-08-22 EP EP95201845A patent/EP0688782B1/en not_active Expired - Lifetime
- 1988-08-22 AT AT95201846T patent/ATE202113T1/de not_active IP Right Cessation
- 1988-08-22 EP EP94202041A patent/EP0630905B1/en not_active Expired - Lifetime
- 1988-08-22 ES ES88307750T patent/ES2113845T3/es not_active Expired - Lifetime
- 1988-08-22 DE DE3856158T patent/DE3856158T2/de not_active Expired - Lifetime
- 1988-08-22 AT AT95201845T patent/ATE217009T1/de not_active IP Right Cessation
- 1988-08-22 CA CA000575329A patent/CA1324128C/en not_active Expired - Lifetime
- 1988-08-22 AT AT94202041T patent/ATE179713T1/de not_active IP Right Cessation
- 1988-08-22 AT AT88307750T patent/ATE164847T1/de not_active IP Right Cessation
- 1988-08-22 IL IL87517A patent/IL87517A/xx not_active IP Right Cessation
- 1988-08-22 ES ES95201845T patent/ES2176279T3/es not_active Expired - Lifetime
- 1988-08-22 EP EP88307750A patent/EP0306190B1/en not_active Expired - Lifetime
- 1988-08-22 EP EP95201846A patent/EP0688783B1/en not_active Expired - Lifetime
- 1988-08-22 DE DE3856527T patent/DE3856527T2/de not_active Expired - Lifetime
- 1988-08-22 DE DE3856477T patent/DE3856477T2/de not_active Expired - Fee Related
- 1988-08-22 ES ES94202041T patent/ES2131152T3/es not_active Expired - Lifetime
- 1988-08-22 DE DE3856330T patent/DE3856330T2/de not_active Expired - Lifetime
- 1988-08-26 HU HU884471A patent/HU202249B/hu unknown
- 1988-08-26 HU HU906268A patent/HU206886B/hu unknown
- 1988-08-26 JP JP63213482A patent/JP2738540B2/ja not_active Expired - Lifetime
- 1988-08-26 IE IE260888A patent/IE81131B1/en not_active IP Right Cessation
- 1988-08-27 KR KR1019880010908A patent/KR970002659B1/ko not_active Expired - Fee Related
-
1992
- 1992-05-27 HU HU9201768A patent/HU9201768D0/hu unknown
-
1997
- 1997-08-25 JP JP9227946A patent/JP2777359B2/ja not_active Expired - Lifetime
- 1997-08-25 JP JP9227948A patent/JP2810034B2/ja not_active Expired - Lifetime
- 1997-08-25 JP JP9227952A patent/JP2899576B2/ja not_active Expired - Lifetime
- 1997-08-25 JP JP9227954A patent/JP2899577B2/ja not_active Expired - Lifetime
-
1998
- 1998-04-10 GR GR980400807T patent/GR3026611T3/el unknown
Also Published As
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG2A | Definitive protection |
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