US4041029A
Expired / Lapsed
US
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Acylimine cephalosporins
Assignee: Merck and Co Inc
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Filing: 1975-09-23
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Granted: 1977-08-09
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Expires: 1995-09-23
Abstract
Abstract A process is provided which yields derivatives of cephalosporins and penicillins. The process starts with 7-acylaminocephalosporin, or 6-acylaminopenicillin, then the latter compounds are treated with an organolithium compound, followed with t-butyl-hypochlorite. Finally, a defined reagent is added yielding a side chain on the carbon adjacent to the amino-nitrogen. Novel intermediate compounds are also described. The end compounds prepared are active against both gram-positive and gram-negative bacteria.
Inventors
- 👤 Raymond A. Firestone
- 👤 Lovji D. Cama
- 👤 Burton G. Christensen
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 11:42
CPC Classifications
C; C07; C07D; C07D499/00; A; A61; A61P; A61P31/00; A61P31/04
Claims Analysis
Total Claims: 6
Claim 1
Independent Claim
52 words
The compound ##STR12## wherein R is phenyl or a 5-membered heterocyclic ring having one O or one S hetero atom; X is hydrogen, amino, or carboxyl; M' is benzyl, benzhydryl, trimethylsilyl, trichloroethyl, methoxymethyl, benzoylmethyl, or methoxybenzyl; and A is hydrogen, loweralkanoyloxy, carbamoyloxy, thiocarbamoyloxy, N-loweralkylcarbamoyloxy, N-loweralkylthiocarbamoyloxy, N,N-diloweralkylcarbamoyloxy, N,N-diloweralkylthiocarbamoyloxy, pyridinium, alkylpyridinium, halopyridinium, or aminopyridinium.
Claim 2
Dependent Claim
52 words
The compound ##STR12## wherein R is phenyl or a 5-membered heterocyclic ring having one O or one S hetero atom; X is hydrogen, amino, or carboxyl; M' is benzyl, benzhydryl, trimethylsilyl, trichloroethyl, methoxymethyl, benzoylmethyl, or methoxybenzyl; and A is hydrogen, loweralkanoyloxy, carbamoyloxy, thiocarbamoyloxy, N-loweralkylcarbamoyloxy, N-loweralkylthiocarbamoyloxy, N,N-diloweralkylcarbamoyloxy, N,N-diloweralkylthiocarbamoyloxy, pyridinium, alkylpyridinium, halopyridinium, or aminopyridinium.
Claim 3
Dependent Claim
13 words
The compound of claim 1 in which R is phenyl, thienyl, or furyl.
Claim 4
Dependent Claim
13 words
The compound of claim 2 in which A is loweralkanoyloxy, carbamoyloxy, or pyridinium.
Claim 5
Dependent Claim
12 words
The compound of claim 3 in which A is acetoxy or carbamoyloxy.
Claim 6
Dependent Claim
18 words
The compound of claim 1 in which X is hydrogen or carboxyl and R is phenyl or thienyl.
References Cited (Backward Citations)
US3778432A
Cited
US3994885A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1980-08-08 | 1981-02-07 | 1981-08-09 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-08-08 | 1985-02-07 | 1985-08-09 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-08-08 | 1989-02-07 | 1989-08-09 | $7700.00 | Window Closed / Lapsed |