# US 4,393,205 A · Cephapirine esters and salts thereof

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 4,393,205 A
- Document ID: US4393205A
- Status: Granted
- Kind: A
- Application number: 06/240,945
- Filed: 1981-03-05
- Granted: 1983-07-12
- Earliest claimed: 1980-03-14
- Assignees: Dobfar S.p.A.
- Inventors: Marco Falciani; Renato Broggi
- Web page: https://patentgrep.com/patent/US4393205A

## CPC

- C07D 501/34: with the 7-amino radical acylated by carboxylic acids containing hetero rings
- A61P 31/04: Antibacterial agents
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Cephapirine esters having the formula ##STR1## wherein R is selected from the group consisting of ##STR2## Such esters and salts thereof, having antibiotic activity, are prepared by reacting 7-ACA with bromophtalide or chloromethylpivalate in the presence of an alkylamine, at a temperature in the range of 0.degree.-70.degree. C. The reaction compound is reacted with chlorohydrate chloride of 4-piridylthioacetic acid. A salt of the compound of formula (I) is isolated from the reaction mixture, after washing with acidic water and addition of a pharmaceutically acceptable acid, by treatment with a suitable solvent.

## Claims

### Claim 1

Cephapirine esters having the formula ##STR6## wherein R is
--CH.sub.2 OCOC(CH.sub.3).sub.3.

### Claim 2 (depends on 1)

Pharmaceutically acceptable salts of the esters of formula (I) of claim 1.

### Claim 3 (depends on 1)

Pharmaceutically acceptable salts of the esters of formula (I) of claim 1, selected from the group consisting of chlorohydrates, p-toluen sulphonates and .beta.-naphthalin-sulphonates of such esters.