US3843641A
Expired / Lapsed
US
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Process for preparing penicillin and cephalosporin compounds
Assignee: Merck and Co Inc
•
Filing: 1972-08-02
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Granted: 1974-10-22
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Expires: 1992-08-02
Abstract
Abstract A process is provided which yields 7-R1 or 6-R1 derivatives of cephalosporins or penicillins, respectively, wherein R1 is methoxy, azido, cyano, fluoro, or chloro. The starting material is a 7-imino, 7-halo, or 6-imino, 6-halo cephalosporin or penicillin which is reacted with a suitable reagent to form the desired side chain derivative. The 7-imino side chain is then removed in the optional presence of a metal catalyst and treatment with an acylating agent yields the final 7-acylamino-7methoxy cephalosporins or the corresponding 6-substituted penicillins. The end products are active antibacterial agents.
Inventors
- 👤 B Christensen
- 👤 L Cama
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 23:47
CPC Classifications
C; C07; C07D; C07D499/00; A; A61; A61P; A61P31/00; A61P31/04
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
9 words
THE PROCESS OF PREPARING THE COMPOUND HAVING THE FORMULA:
Claim 2
Dependent Claim
9 words
THE PROCESS OF PREPARING THE COMPOUND HAVING THE FORMULA:
Claim 3
Dependent Claim
19 words
The process of claim 1 wherein the metal catalyst is employed in the reaction with the substituted acetyl chloride.
Claim 4
Dependent Claim
14 words
The process of claim 2 wherein the metal catalyst is palladium or platinum halide.
Claim 5
Dependent Claim
11 words
The process of claim 3 wherein the catalyst is palladious chloride.
Claim 6
Dependent Claim
26 words
The process of claim 1 wherein the metal catalyst is employed in an amount equivalent to about 1/2 to 1 molar equivalents of the methoxy-imino compound.
Claim 7
Dependent Claim
16 words
The process of claim 1 wherein R is phenyl, furyl, or thienyl, and X is hydrogen.
Claim 8
Dependent Claim
10 words
The process of claim 6 wherein (Z) is the group
Claim 9
Dependent Claim
15 words
The process of claim 7 wherein A is lower-alkanoyloxy of 1-6 carbon atoms, or carbamoyloxy.
Claim 10
Dependent Claim
11 words
The process of claim 8 wherein A is acetoxy or carbamoyloxy.
Claim 11
Dependent Claim
9 words
The process of claim 9 wherein A is carbamoyloxy.
Claim 12
Dependent Claim
9 words
The process of claim 10 wherein R is 2-thienyl.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1977-10-21 | 1978-04-22 | 1978-10-22 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1981-10-21 | 1982-04-22 | 1982-10-22 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1985-10-21 | 1986-04-22 | 1986-10-22 | $7700.00 | Window Closed / Lapsed |