Novel ampicillin esters and production thereof

Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Parasitic organism or component thereof or substance...

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Details

2602391, 2602452R, A61K 3143, C07D49932, C07D49942

Patent

active

043894089

ABSTRACT:
A novel Ampicillin ester of the general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, a methyl group or an aryl group, and R.sub.2 represents a hydrogen atom or may be taken together with R.sub.1 to form a divalent carbon chain residue, or its acid addition salt.
The novel Ampicillin ester or its acid addition salt is prepared by (1) reacting a corresponding 6-N-acylamino penicillanic acid (II) or its salt with a compound of the formula ##STR2## wherein R.sub.1 and R.sub.2 are as defined above, and X is a halogen atom, or reacting a compound of the formula ##STR3## wherein R.sub.1 and R.sub.2 are as defined above, or its acid addition salt with a corresponding carboxylic acid (VI) or its reactive derivative, (2) thereafter, if required, when the resulting compound has the protected amino group or the group convertible to an amino group, deprotecting the protected amino group or converting said convertible group to an amino group, and (3) if further required, converting the product to an acid addition salt.
The present invention provides also an antibacterial agent comprising the novel Ampicillin ester and a method for the treatment of infectious disease.

REFERENCES:
patent: 3951954 (1976-04-01), Murakami et al.

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