US3901942A
Expired / Lapsed
US
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Tetracycline derivatives substituted in the 7 position and process for preparing the same
Assignee: Pfizer Italia SRL
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Filing: 1973-09-17
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Granted: 1975-08-26
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Expires: 1993-09-17
Abstract
Abstract Process for the preparation of tetracycline derivatives substituted in the 7 position comprising first obtaining tetracycline derivatives substituted in the 7 and 9 positions, transforming the substituent in the 7 position into the desired substituent, and then eliminating the substituent in the 9 position. Invention further comprises products obtained during the course of the above process.
Inventors
- 👤 Luigi Bernardi
- 👤 Vincenzo Colonna
- 👤 Roberto De Castiglione
- 👤 Paolo Masi
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 07:32
CPC Classifications
C; C07; C07C; C07C233/00; A; A61; A61P; A61P31/00; A61P31/04; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 6
Claim 1
Independent Claim
12 words
A PROCESS FOR THE PREPARATION OF A COMPOUND OF THE FORMULA (VII)
Claim 2
Dependent Claim
12 words
A PROCESS FOR THE PREPARATION OF A COMPOUND OF THE FORMULA (VII)
Claim 3
Dependent Claim
40 words
THE PROCESS OF CLAIM FURTHER COMPRISING DISSOLVING SAID COMPOUND (VII) IN A SOLVENT, EFFECTING CATALYTIC REDUCTION IN THE PRESENCE OF AN ALDEHYDE AND A KETONE HAVING FROM 1 TO 4 CARBON ATOMS TO FORM A COMPOUND OF THE FORMULA (VIII)
Claim 4
Dependent Claim
31 words
The process of claim 1 further comprising dissolving said 9-t.butyl-7-nitro-6-demethyl-6-deoxytetracycline in an alcohol and effecting alkylating reduction in the presence of formaldehyde and a noble metal catalyst to thereby obtain 9-t.butyl-7-dimethylamino-6-demethyl-6-deoxytetracycline.
Claim 5
Dependent Claim
12 words
The process of claim 3 wherein said catalyst is platinum or palladium.
Claim 6
Dependent Claim
41 words
The process of claim 3, further comprising treating said 9-t.butyl-7-dimethylamino-6-demethyl-6-deoxytetracycline with trifluoromethansulfonic acid to eliminate the t.butyl group in the 9 position, isolating the resulting 7-dimethyl-amino-6-demethyl-6-deoxytetracycline, and subsequently transforming this product into its salt by reaction with a pharmaceutically acceptable acid.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1978-08-25 | 1979-02-24 | 1979-08-26 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1982-08-25 | 1983-02-24 | 1983-08-26 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1986-08-25 | 1987-02-24 | 1987-08-26 | $7700.00 | Window Closed / Lapsed |