SE8603309L - INTERMEDIATES FOR PENICILLANIC ACID-1,1-DIOXIDE PREPARATION AND ESTERS THEREOF - Google Patents
INTERMEDIATES FOR PENICILLANIC ACID-1,1-DIOXIDE PREPARATION AND ESTERS THEREOFInfo
- Publication number
- SE8603309L SE8603309L SE8603309A SE8603309A SE8603309L SE 8603309 L SE8603309 L SE 8603309L SE 8603309 A SE8603309 A SE 8603309A SE 8603309 A SE8603309 A SE 8603309A SE 8603309 L SE8603309 L SE 8603309L
- Authority
- SE
- Sweden
- Prior art keywords
- penicillanic acid
- esters
- vivo
- dioxide
- readily hydrolyzable
- Prior art date
Links
- FKENQMMABCRJMK-RITPCOANSA-N sulbactam Chemical compound O=S1(=O)C(C)(C)[C@H](C(O)=O)N2C(=O)C[C@H]21 FKENQMMABCRJMK-RITPCOANSA-N 0.000 title abstract 4
- 239000000543 intermediate Substances 0.000 title abstract 2
- 150000002148 esters Chemical class 0.000 abstract 4
- 238000001727 in vivo Methods 0.000 abstract 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 125000001475 halogen functional group Chemical group 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 208000035143 Bacterial infection Diseases 0.000 abstract 1
- 241000124008 Mammalia Species 0.000 abstract 1
- 229930182555 Penicillin Natural products 0.000 abstract 1
- 208000022362 bacterial infectious disease Diseases 0.000 abstract 1
- 239000003782 beta lactam antibiotic agent Substances 0.000 abstract 1
- 239000003781 beta lactamase inhibitor Substances 0.000 abstract 1
- 229940126813 beta-lactamase inhibitor Drugs 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 238000005695 dehalogenation reaction Methods 0.000 abstract 1
- 230000002708 enhancing effect Effects 0.000 abstract 1
- 238000007327 hydrogenolysis reaction Methods 0.000 abstract 1
- RBKMMJSQKNKNEV-RITPCOANSA-N penicillanic acid Chemical class OC(=O)[C@H]1C(C)(C)S[C@@H]2CC(=O)N21 RBKMMJSQKNKNEV-RITPCOANSA-N 0.000 abstract 1
- 150000002960 penicillins Chemical class 0.000 abstract 1
- 239000002132 β-lactam antibiotic Substances 0.000 abstract 1
- 229940124586 β-lactam antibiotics Drugs 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D499/00—Heterocyclic compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. penicillins, penems; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
-
- 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
- A61P31/04—Antibacterial agents
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Communicable Diseases (AREA)
- Pharmacology & Pharmacy (AREA)
- Oncology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Cosmetics (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Abstract
A process for the preparation of penicillanic acid 1,1-dioxide and esters thereof readily hydrolyzable in vivo. Said process involves dehalogenation of a 6-halo or 6,6-dihalo derivative of penicillanic acid 1,1-dioxide or ester thereof readily hydrolyzable in vivo or a carboxy protected derivative thereof (e.g. by hydrogenolysis). The 6-halo and 6,6-dihalo derivatives of penicillanic acid 1,1-dioxides, esters thereof readily hydrolyzable in vivo, and carboxy protected derivatives thereof are novel intermediates. Penicillanic acid 1,1-dioxide, and esters thereof readily hydrolyzable in vivo, are known compounds which are useful as beta- lactamase inhibitors and for enhancing the effectiveness of certain beta-lactam antibiotics (e.g. the penicillins) in the treatment of bacterial infections in mammals, particularly humans.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US1781079A | 1979-03-05 | 1979-03-05 | |
| US1780879A | 1979-03-05 | 1979-03-05 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| SE8603309D0 SE8603309D0 (en) | 1986-08-04 |
| SE8603309L true SE8603309L (en) | 1986-08-04 |
Family
ID=26690337
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SE8000512A SE449103B (en) | 1979-03-05 | 1980-01-22 | SET TO PENICILLANIC ACID-1,1-DIOXIDE AND ESSERS THEREOF |
| SE8603309A SE8603309L (en) | 1979-03-05 | 1986-08-04 | INTERMEDIATES FOR PENICILLANIC ACID-1,1-DIOXIDE PREPARATION AND ESTERS THEREOF |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SE8000512A SE449103B (en) | 1979-03-05 | 1980-01-22 | SET TO PENICILLANIC ACID-1,1-DIOXIDE AND ESSERS THEREOF |
Country Status (36)
| Country | Link |
|---|---|
| KR (1) | KR850001339B1 (en) |
| AR (1) | AR225031A1 (en) |
| AT (1) | AT366693B (en) |
| AU (1) | AU522572B2 (en) |
| BG (1) | BG33292A3 (en) |
| CH (1) | CH644608A5 (en) |
| CS (1) | CS215130B2 (en) |
| DD (1) | DD149367A5 (en) |
| DE (1) | DE3008257C2 (en) |
| DK (2) | DK159852C (en) |
| EG (1) | EG14437A (en) |
| ES (1) | ES489185A0 (en) |
| FI (1) | FI70024C (en) |
| FR (1) | FR2450836B1 (en) |
| GB (1) | GB2045755B (en) |
| GR (1) | GR67234B (en) |
| HK (1) | HK66587A (en) |
| HU (1) | HU186304B (en) |
| IE (1) | IE49535B1 (en) |
| IL (1) | IL59515A (en) |
| IN (1) | IN153685B (en) |
| IT (1) | IT1130300B (en) |
| KE (1) | KE3464A (en) |
| LU (1) | LU82215A1 (en) |
| MX (1) | MX6032E (en) |
| MY (1) | MY8500319A (en) |
| NL (1) | NL180317C (en) |
| NO (2) | NO800618L (en) |
| PL (1) | PL125197B1 (en) |
| PT (1) | PT70897A (en) |
| RO (1) | RO80112A (en) |
| SE (2) | SE449103B (en) |
| SG (1) | SG55884G (en) |
| SU (1) | SU1192626A3 (en) |
| UA (1) | UA6342A1 (en) |
| YU (1) | YU42328B (en) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4419284A (en) * | 1981-03-23 | 1983-12-06 | Pfizer Inc. | Preparation of halomethyl esters (and related esters) of penicillanic acid 1,1-dioxide |
| IN159362B (en) * | 1981-03-23 | 1987-05-09 | Pfizer | |
| US4360463A (en) | 1981-09-02 | 1982-11-23 | Pfizer Inc. | Pure 6,6-diiodopenicillanic acid and process for its preparation |
| PT76527B (en) * | 1982-04-19 | 1985-12-09 | Gist Brocades Nv | A process for the preparation of penicillanic acid 1,1-dioxide and derivatives thereof |
| IT1190897B (en) * | 1982-06-29 | 1988-02-24 | Opos Biochimica Srl | PROCEDURE FOR THE PREPARATION OF THE 1-ETHOXYCARBONYLOXYETHYL ACID ACID 6- (D (-) - ALPHA AMINOALPHA-PHENYLACETAMIDE) -PENICILLANIC |
| US4606865A (en) * | 1982-09-20 | 1986-08-19 | Astra Lakemedel Aktiebolag | Methods for the preparation of α-bromodiethylcarbonate |
| EP0139048A1 (en) * | 1983-10-18 | 1985-05-02 | Gist-Brocades N.V. | Process for the dehalogenation of 6,6-dibromopenicillanic acid 1,1-dioxide |
| EP0139047A1 (en) * | 1983-10-18 | 1985-05-02 | Gist-Brocades N.V. | Process for the preparation of 6,6-dibromopenicillanic acid 1,1-dioxide |
| US4596677A (en) * | 1984-04-06 | 1986-06-24 | Bristol-Myers Company | Anhydropenicillin intermediates |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IN149747B (en) * | 1977-06-07 | 1982-04-03 | Pfizer | |
| CA1158639A (en) * | 1978-12-11 | 1983-12-13 | Eric M. Gordon | 6-bromopenicillanic acid sulfone |
| EP0013617B1 (en) * | 1979-01-10 | 1984-07-04 | Beecham Group Plc | Penicillin derivatives, process for their preparation and pharmaceutical compositions containing certain of these compounds |
| IE49880B1 (en) * | 1979-02-13 | 1986-01-08 | Leo Pharm Prod Ltd | Penicillin derivatives |
-
1980
- 1980-01-22 SE SE8000512A patent/SE449103B/en not_active IP Right Cessation
- 1980-02-11 IN IN98/DEL/80A patent/IN153685B/en unknown
- 1980-02-27 SU SU802889601A patent/SU1192626A3/en active
- 1980-02-27 UA UA2889601A patent/UA6342A1/en unknown
- 1980-02-29 HU HU80479A patent/HU186304B/en unknown
- 1980-03-03 AR AR280148A patent/AR225031A1/en active
- 1980-03-03 YU YU585/80A patent/YU42328B/en unknown
- 1980-03-03 LU LU82215A patent/LU82215A1/en unknown
- 1980-03-03 IL IL59515A patent/IL59515A/en unknown
- 1980-03-03 GB GB8007122A patent/GB2045755B/en not_active Expired
- 1980-03-04 ES ES489185A patent/ES489185A0/en active Granted
- 1980-03-04 RO RO80100366A patent/RO80112A/en unknown
- 1980-03-04 GR GR61347A patent/GR67234B/el unknown
- 1980-03-04 AU AU56104/80A patent/AU522572B2/en not_active Expired
- 1980-03-04 CH CH171080A patent/CH644608A5/en not_active IP Right Cessation
- 1980-03-04 EG EG123/80A patent/EG14437A/en active
- 1980-03-04 FI FI800661A patent/FI70024C/en not_active IP Right Cessation
- 1980-03-04 CS CS801496A patent/CS215130B2/en unknown
- 1980-03-04 PL PL1980222448A patent/PL125197B1/en unknown
- 1980-03-04 DK DK092680A patent/DK159852C/en not_active IP Right Cessation
- 1980-03-04 NL NLAANVRAGE8001285,A patent/NL180317C/en not_active IP Right Cessation
- 1980-03-04 KR KR1019800000885A patent/KR850001339B1/en not_active Expired
- 1980-03-04 DE DE3008257A patent/DE3008257C2/en not_active Expired
- 1980-03-04 DD DD80219432A patent/DD149367A5/en unknown
- 1980-03-04 PT PT70897A patent/PT70897A/en unknown
- 1980-03-04 NO NO800618A patent/NO800618L/en unknown
- 1980-03-04 IE IE429/80A patent/IE49535B1/en not_active IP Right Cessation
- 1980-03-04 FR FR8004764A patent/FR2450836B1/en not_active Expired
- 1980-03-04 AT AT0119080A patent/AT366693B/en not_active IP Right Cessation
- 1980-03-05 BG BG046874A patent/BG33292A3/en unknown
- 1980-03-05 IT IT20367/80A patent/IT1130300B/en active
- 1980-03-05 MX MX808687U patent/MX6032E/en unknown
-
1982
- 1982-09-15 NO NO823127A patent/NO823127L/en unknown
-
1984
- 1984-08-13 SG SG558/84A patent/SG55884G/en unknown
- 1984-09-24 KE KE3464A patent/KE3464A/en unknown
-
1985
- 1985-12-30 MY MY319/85A patent/MY8500319A/en unknown
-
1986
- 1986-08-04 SE SE8603309A patent/SE8603309L/en not_active Application Discontinuation
-
1987
- 1987-09-17 HK HK665/87A patent/HK66587A/en not_active IP Right Cessation
-
1990
- 1990-06-14 DK DK145690A patent/DK166353C/en not_active IP Right Cessation
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| NAV | Patent application has lapsed |
Ref document number: 8603309-9 Effective date: 19900713 |